US2002173645A1PendingUtilityA1

Non-solvated crystalline 6-hydroxy-2- (4-hydroxyphenyl) -3- [4- (2-piperidinoethoxy) benzoyl] benzo [b] thiophene hydrochloride

Priority: Sep 19, 1994Filed: Feb 26, 2002Published: Nov 21, 2002
Est. expirySep 19, 2014(expired)· nominal 20-yr term from priority
A61P 5/24A61P 43/00C07D 333/56A61P 15/18C07D 409/10
51
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Claims

Abstract

The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxy)benzoyl]benzo[b]-thiophenes. The present invention is also directed to crystalline solvates and a non-solvated crystalline form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride, as well as processes for their preparation.

Claims

exact text as granted — not AI-modified
We claim:  
     
         1 . A process for preparing a crystalline solvate of a compound of the formula  
       
         
           
           
               
               
           
         
         wherein: 
 R 1  is hydrogen or hydroxyl;  
 R 2  and R 3  are independently C 1 -C 4  alkyl, or R 2  and R 3  together with the adjacent nitrogen atom form a heterocyclic ring selected from the group consisting of pyrrolidino, piperidino, hexamethyleneimino, and morpholino; and  
 HX is HCl or HBr;  
 comprising the steps of:  
 
         (a) acylating a benzothiophene of the formula  
         
           
             
             
                 
                 
             
           
         
         wherein: 
 R 4  is hydrogen or C 1 -C 4  alkoxy, and  
 R 5  is C 1 -C 4  alkyl,  
 
         with an acylating agent of the formula  
         
           
             
             
                 
                 
             
           
         
         wherein: 
 R 6  is chloro, bromo, or hydroxyl, and  
 HX, R 2 , and R 3  are as defined above,  
 
         in the presence of BX′ 3 , wherein X′ is chloro or bromo;  
         (b) dealkylating one or more phenolic groups of the acylation product of step (a) by reacting with additional BX 3 ′, wherein X′ is as defined above; and  
         (c) isolating the crystalline solvate.  
       
     
     
         2 . The process of  claim 1  wherein R 6  is chloro and HX is HCl.  
     
     
         3 . The process of  claim 2  wherein R 1  is hydroxyl and R 4  is C 1 -C 4  alkoxy.  
     
     
         4 . The process of  claim 3  wherein R 2  and R 3  together with the adjacent nitrogen atom form a heterocyclic ring selected from the group consisting of pyrrolidino, piperidino, and hexamethyleneimino.  
     
     
         5 . The process of  claim 4  wherein X′ is chloro.  
     
     
         6 . The process of  claim 5  wherein R 4  is methoxy and R 5  is methyl.  
     
     
         7 . The process of  claim 6  wherein R 2  and R 3  together with the adjacent nitrogen atom form a piperidino group.  
     
     
         8 . The process of  claim 7  wherein the acylation is conducted in the presence of 2-5 molar equivalents of BCl 3 .  
     
     
         9 . The process of  claim 7  wherein the dealkylation is conducted in presence of 3-10 molar equivalents of BCl 3 .  
     
     
         10 . The process of  claim 7  wherein the reaction solvent is one or more solvents selected from the group consisting of chloroform, methylene chloride, 1,2-dichloroethane, 1,2,3-trichloropropane, 1,1,2,2-tetrachloroethane, 1,2-dichlorobenzene, chlorobenzene, and fluorobenzene.  
     
     
         11 . The process of  claim 7  wherein the reaction solvent is 1,2-dichloroethane.  
     
     
         12 . A process for preparing a compound of the formula  
       
         
           
           
               
               
           
         
         or the hydrochloride or hydrobromide salt thereof, wherein: 
 R 4  is hydrogen or C 1 -C 4  alkoxy;  
 R 5  is C 1 -C 4  alkyl; and  
 R 2  and R 3  are independently C 1 -C 4  alkyl, or R 2  and R 3  together with the adjacent nitrogen atom form a heterocyclic ring selected from the group consisting of pyrrolidino, piperidino, hexamethyleneimino, and morpholino;  
 comprising acylating a benzothiophene of the formula  
                     
 
         wherein: 
 R 4  and R 5  are as defined above,  
 
         with an acylating agent of the formula  
         
           
             
             
                 
                 
             
           
         
         wherein: 
 R 6  is chloro, bromo, or hydroxyl;  
 R 2  and R 3  are independently C 1 -C 4  alkyl, or R 2  and R 3  together with the adjacent nitrogen atom form a heterocyclic ring selected from the group consisting of pyrrolidino, piperidino, hexamethyleneimino, and morpholino; and  
 HX is HCl or HBr;  
 in the presence of BX′ 3 , wherein X′ is chloro or bromo.  
 
       
     
     
         13 . The process of  claim 12  wherein R 6  is chloro and HX is HCl.  
     
     
         14 . The process of  claim 13  wherein R 4  is C 1 -C 4  alkoxy.  
     
     
         15 . The process of  claim 14  wherein R 2  and R 3  together with the adjacent nitrogen atom form a heterocyclic ring selected from the group consisting of pyrrolidino, piperidino, and hexamethyleneimino.  
     
     
         16 . The process of  claim 15  wherein X′ is chloro.  
     
     
         17 . The process of  claim 16  wherein R 4  is methoxy, and R 5  is methyl.  
     
     
         18 . The process of  claim 17  wherein R 2  and R 3  together with the adjacent nitrogen atom form a piperidino group.  
     
     
         19 . The process of  claim 18  wherein the acylation is conducted in the presence of 2-5 molar equivalents of BCl 3 .  
     
     
         20 . The process of  claim 18  wherein the reaction solvent is one or more solvents selected from the group consisting of chloroform, methylene chloride, chlorobenzene, 1,2-dichloroethane, 1,2,3-trichloropropane, 1,1,2,2-tetrachloroethane, 1,2-dichlorobenzene, bromobenzene, and fluorobenzene.  
     
     
         21 . The process of  claim 18  wherein the reaction solvent is methylene chloride.  
     
     
         22 . A process for preparing a crystalline solvate of a compound of the formula  
       
         
           
           
               
               
           
         
         wherein 
 R 1  is hydrogen or hydroxyl;  
 R 2  and R 3  are independently C 1 -C 4  alkyl, or R 2  and R 3  together with the adjacent nitrogen atom form a heterocyclic ring selected from the group consisting of pyrrolidino, piperidino, hexamethyleneimino, and morpholino; and  
 HX is HCl or HBr;  
 comprising (a) dealkylation of one or more of the phenolic groups of a compound of the formula  
                     
 
         wherein: 
 R 4  is hydrogen or C 1 -C 4  alkoxy;  
 R 5  is C 1 -C 4  alkyl; and  
 HX, R 2 , and R 3  are as defined above;  
 
         by reacting with BX′ 3 , wherein X′ is chloro or bromo; and  
         (b) isolating the crystalline solvate.  
       
     
     
         23 . The process of  claim 22  wherein X′ is chloro and HX is HCl.  
     
     
         24 . The process of  claim 23  wherein R 1  is hydroxyl and R 4  is C 1 -C 4  alkoxy.  
     
     
         25 . The process of  claim 24  wherein R 2  and R 3  together with the adjacent nitrogen atom form a heterocyclic ring selected from the group consisting of pyrrolidino, piperidino, and hexamethyleneimino.  
     
     
         26 . The process of  claim 25  wherein R 4  is methoxy and R 5  is methyl.  
     
     
         27 . The process of  claim 26  wherein R 2  and R 3  together with the adjacent nitrogen atom form a piperidino group.  
     
     
         28 . The process of  claim 27  wherein the reaction solvent is one or more solvents selected from the group consisting of methylene chloride, chlorobenzene, 1,2-dichloroethane, chloroform, 1,1,2,2-tetrachloroethane, 1,2,3-trichloropropane, 1,2-dichlorobenzene, and fluorobenzene.  
     
     
         29 . The process of  claim 27  wherein the reaction solvent is 1,2-dichloroethane.  
     
     
         30 . A crystalline solvate of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene hydrochloride having the following X-ray diffraction pattern obtained with copper radiation:  
       
         
           
                 
                 
                 
               
                     
                     
                 
                     
                     
                 
                     
                   d-line spacing 
                   I/I o   
                 
                     
                   (Angstroms) 
                   (×100) 
                 
                     
                     
                 
                     
                 
                 
                 
                 
               
                     
                   10.4311 
                   22.64 
                 
                     
                   8.9173 
                   10.73 
                 
                     
                   8.4765 
                   5.31 
                 
                     
                   8.0095 
                   50.39 
                 
                     
                   7.3068 
                   4.23 
                 
                     
                   6.6094 
                   79.23 
                 
                     
                   5.6196 
                   22.34 
                 
                     
                   5.4223 
                   89.86 
                 
                     
                   5.1959 
                   11.81 
                 
                     
                   5.0746 
                   74.90 
                 
                     
                   4.8017 
                   100.00 
                 
                     
                   4.7262 
                   57.97 
                 
                     
                   4.6569 
                   53.35 
                 
                     
                   4.5378 
                   96.75 
                 
                     
                   4.4376 
                   10.83 
                 
                     
                   4.3397 
                   56.89 
                 
                     
                   4.2782 
                   48.23 
                 
                     
                   4.2129 
                   40.94 
                 
                     
                   4.1037 
                   12.80 
                 
                     
                   3.9880 
                   14.76 
                 
                     
                   3.8863 
                   8.17 
                 
                     
                   3.7999 
                   42.13 
                 
                     
                   3.7662 
                   57.09 
                 
                     
                   3.6738 
                   38.58 
                 
                     
                   3.5701 
                   18.50 
                 
                     
                   3.5393 
                   19.00 
                 
                     
                   3.4622 
                   39.57 
                 
                     
                   3.3867 
                   5.02 
                 
                     
                   3.3321 
                   4.33 
                 
                     
                   3.2686 
                   6.79 
                 
                     
                   3.1535 
                   14.86 
                 
                     
                   3.0450 
                   13.58 
                 
                     
                   2.9028 
                   12.30 
                 
                     
                   2.8302 
                   19.59 
                 
                     
                   2.7544 
                   12.30 
                 
                     
                   2.6366 
                   6.89 
                 
                     
                     
                 
                     
                     
                 
             
                
                
                
                
                
               
               
                
               
            
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         31 . The crystalline solvate of  claim 30  which is a 1,2-dichloroethane solvate.  
     
     
         32 . The crystalline solvate of  claim 30  which is a 1,2,3-trichloropropane solvate.  
     
     
         33 . A crystalline solvate of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene hydrochloride having the following X-ray diffraction pattern obtained with copper radiation:  
       
         
           
                 
                 
                 
               
                     
                     
                 
                     
                     
                 
                     
                   d-line spacing 
                   I/I o   
                 
                     
                   (Angstroms) 
                   (×100) 
                 
                     
                     
                 
                     
                 
                 
                 
                 
               
                     
                   16.1265 
                   3.80 
                 
                     
                   10.3744 
                   8.63 
                 
                     
                   8.3746 
                   5.29 
                 
                     
                   7.9883 
                   36.71 
                 
                     
                   7.2701 
                   5.06 
                 
                     
                   6.5567 
                   70.77 
                 
                     
                   6.2531 
                   6.79 
                 
                     
                   5.5616 
                   24.05 
                 
                     
                   5.3879 
                   100.00 
                 
                     
                   5.0471 
                   89.64 
                 
                     
                   4.7391 
                   85.96 
                 
                     
                   4.6777 
                   39.36 
                 
                     
                   4.6332 
                   62.60 
                 
                     
                   4.5191 
                   77.56 
                 
                     
                   4.2867 
                   36.82 
                 
                     
                   4.2365 
                   41.66 
                 
                     
                   4.1816 
                   49.60 
                 
                     
                   4.0900 
                   11.28 
                 
                     
                   3.9496 
                   11.85 
                 
                     
                   3.7869 
                   36.25 
                 
                     
                   3.7577 
                   56.16 
                 
                     
                   3.6509 
                   40.62 
                 
                     
                   3.5751 
                   15.65 
                 
                     
                   3.5181 
                   21.52 
                 
                     
                   3.4964 
                   18.53 
                 
                     
                   3.4361 
                   33.60 
                 
                     
                   3.3610 
                   6.21 
                 
                     
                   3.3115 
                   4.95 
                 
                     
                   3.2564 
                   7.36 
                 
                     
                   3.2002 
                   3.80 
                 
                     
                   3.1199 
                   15.77 
                 
                     
                   3.0347 
                   14.84 
                 
                     
                   2.8744 
                   9.67 
                 
                     
                   2.8174 
                   10.82 
                 
                     
                   2.7363 
                   11.51 
                 
                     
                     
                 
                     
                     
                 
             
                
                
                
                
                
               
               
                
               
            
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         34 . The crystalline solvate of  claim 33  which is a 1,2-dichloroethane solvate.  
     
     
         35 . A process for preparing the crystalline solvate of  claim 30 , comprising the steps of: (a) dealkylating the hydrochloride salt of a compound of the formula  
       
         
           
           
               
               
           
         
         wherein R 7  is C 1 -C 4  alkyl,  
         by reacting with BCl 3  in an organic solvent selected from the group consisting of 1,2-dichloroethane and 1,2,3-trichloropropane; (b) quenching the reaction of step (a) with methanol; and (c) isolating the crystalline solvate.  
       
     
     
         36 . The process of  claim 35  wherein the organic solvent is 1,2-dichloroethane.  
     
     
         37 . The process of  claim 36  wherein R 7  is methyl.  
     
     
         38 . The process of  claim 35  wherein the organic solvent is 1,2,3-trichloropropane.  
     
     
         39 . A process for preparing the crystalline solvate of  claim 33 , comprising the steps of: 
 (a) dealkylating the hydrochloride salt of a compound of the formula                          wherein R 7  is C 1 -C 4  alkyl,    by reacting with BCl 3  in 1,2-dichloroethane; (b) quenching the reaction of step (a) with ethanol; and (c) isolating the crystalline solvate.    
     
     
         40 . The process of  claim 39  wherein R 7  is methyl.  
     
     
         41 . A process for preparing a crystalline solvate of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene hydrochloride having the following X-ray diffraction pattern obtained with copper radiation:  
       
         
           
                 
                 
                 
               
                     
                     
                 
                     
                     
                 
                     
                   d-line spacing 
                   I/I o   
                 
                     
                   (Angstroms) 
                   (x100) 
                 
                     
                     
                 
                     
                 
                 
                 
                 
               
                     
                   14.3518 
                   7.24 
                 
                     
                   10.3335 
                   6.17 
                 
                     
                   8.8305 
                   4.29 
                 
                     
                   7.9475 
                   38.16 
                 
                     
                   6.5904 
                   64.25 
                 
                     
                   6.2848 
                   6.52 
                 
                     
                   5.6048 
                   28.06 
                 
                     
                   5.4107 
                   100.00 
                 
                     
                   5.1544 
                   11.26 
                 
                     
                   5.0493 
                   53.26 
                 
                     
                   5.0224 
                   46.11 
                 
                     
                   4.8330 
                   76.94 
                 
                     
                   4.7694 
                   34.23 
                 
                     
                   4.6461 
                   50.22 
                 
                     
                   4.5754 
                   38.61 
                 
                     
                   4.4953 
                   72.65 
                 
                     
                   4.3531 
                   49.15 
                 
                     
                   4.2940 
                   41.64 
                 
                     
                   4.2425 
                   35.75 
                 
                     
                   4.1856 
                   21.63 
                 
                     
                   4.1338 
                   9.47 
                 
                     
                   4.0793 
                   12.69 
                 
                     
                   3.9960 
                   18.50 
                 
                     
                   3.9037 
                   9.03 
                 
                     
                   3.7854 
                   40.39 
                 
                     
                   3.7521 
                   54.16 
                 
                     
                   3.6787 
                   28.60 
                 
                     
                   3.6509 
                   17.96 
                 
                     
                   3.5444 
                   31.72 
                 
                     
                   3.4679 
                   41.55 
                 
                     
                   3.3899 
                   7.69 
                 
                     
                   3.3101 
                   5.72 
                 
                     
                   3.2561 
                   7.42 
                 
                     
                   3.1784 
                   15.19 
                 
                     
                   3.0445 
                   11.17 
                 
                     
                   3.0146 
                   8.94 
                 
                     
                   2.9160 
                   11.89 
                 
                     
                   2.8217 
                   18.23 
                 
                     
                   2.7500 
                   12.06 
                 
                     
                   2.6436 
                   9.65 
                 
                     
                   2.6156 
                   6.97 
                 
                     
                     
                 
                     
                     
                 
             
                
                
                
                
                
               
               
                
               
            
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
         comprising the steps of: 
 (a) dealkylating the hydrochloride salt of a compound of the formula  
                     
 wherein R 7  is C 1 -C 4  alkyl,  
 by reacting with BCl 3  in chlorobenzene;  
 (b) quenching the reaction of step (a) with methanol; and  
 (c) isolating the crystalline solvate.  
 
       
     
     
         42 . The process of  claim 41  wherein R 7  is methyl.  
     
     
         43 . A process for preparing a crystalline solvate of a compound of the formula  
       
         
           
           
               
               
           
         
         wherein: 
 R 1  is hydrogen or hydroxyl;  
 R 2  and R 3  are independently C 1 -C 4  alkyl, or R 2  and R 3  together with the adjacent nitrogen atom form a heterocyclic ring selected from the group consisting of pyrrolidino, piperidino, hexamethyleneimino, and morpholino; and  
 HX is HCl or HBr;  
 comprising the steps of:  
 
         (a) chlorinating with phosgene a compound of the formula  
         
           
             
             
                 
                 
             
           
         
         wherein: 
 HX, R 2 , and R 3  are as defined above, and  
 R 6  is hydroxyl  
 
         to produce a formula III compound wherein R 6  is chloro;  
         (b) acylating a benzothiophene of the formula  
         
           
             
             
                 
                 
             
           
         
         wherein: 
 R 4  is hydrogen or C 1 -C 4  alkoxy, and  
 R 5  is C 1 -C 4  alkyl,  
 
         with a compound of formula III, wherein R 6  is chloro, in the presence of BX′ 3 , wherein X′ is chloro or bromo;  
         (c) dealkylating one or more phenolic groups of the acylation product of step (b) by reacting with additional BX′ 3 , wherein X′ is as defined above; and  
         (d) isolating the crystalline solvate.  
       
     
     
         44 . The process of  claim 43  wherein R 1  is hydroxyl and R 4  is C 1 -C 4  alkoxy.  
     
     
         45 . The process of  claim 44  wherein X′ is chloro and HX is HCl.  
     
     
         46 . The process of  claim 45  wherein R 4  is methoxy and R 5  is methyl.  
     
     
         47 . The process of  claim 46  wherein R 2  and R 3  together with the adjacent nitrogen atom form a piperidino group.  
     
     
         48 . A process for preparing a crystalline solvate of a compound of the formula  
       
         
           
           
               
               
           
         
         wherein: 
 R 1  is hydrogen or hydroxyl;  
 R 2  and R 3  are independently C 1 -C 4  alkyl, or R 2  and R 3  together with the adjacent nitrogen atom form a heterocyclic ring selected from the group consisting of pyrrolidino, piperidino, hexamethyleneimino, and morpholino; and  
 HX is HCl or HBr;  
 comprising the steps of:  
 
         (a) chlorinating a compound of the formula  
         
           
             
             
                 
                 
             
           
         
         wherein: 
 HX, R 2 , and R 3  are as defined above, and  
 R 6  is hydroxyl,  
 
         with a chlorination reagent to produce a formula III compound wherein R 6  is chloro;  
         (b) removing the excess chlorination agent;  
         (c) acylating a benzothiophene of the formula  
         
           
             
             
                 
                 
             
           
         
         wherein: 
 R 4  is hydrogen or C 1 -C 4  alkoxy, and  
 R 5  is C 1 -C 4  alkyl,  
 
         with a compound of formula III, wherein R 6  is chloro, in the presence of BX′3, wherein X′ is chloro or bromo;  
         (d) dealkylating one or more phenolic groups of the acylation product of step (c) by reacting with additional BX′3, wherein X′ is as defined above; and  
         (e) isolating the crystalline solvate.  
       
     
     
         49 . The process of  claim 48  wherein R 1  is hydroxyl and R 4  is C 1 -C 4  alkoxy.  
     
     
         50 . The process of  claim 49  wherein X′ is chloro and HX is HCl.  
     
     
         51 . The process of  claim 50  wherein R 4  is methoxy and R 5  is methyl.  
     
     
         52 . The process of  claim 51  wherein R 2  and R 3  together with the adjacent nitrogen atom form a piperidino group.  
     
     
         53 . A process for preparing the crystalline solvate of  claim 30 , comprising the steps of: 
 (a) acylating a benzothiophene of the formula                          wherein: 
 R 4  is C 1 -C 4  alkoxy and R 5  is C 1 -C 4  alkyl, with an acylating agent of the formula  
                     
   wherein: 
 R 6  is chloro, and R 2  and R 3  together with the adjacent nitrogen atom form a piperidino group, and HX is HCl, in the presence of BCl 3  in an organic solvent selected from the group consisting of 1,2-dichloroethane and 1,2,3-trichloropropane;  
   (b) dealkylating the hydrochloride salt of the compound of the formula                        wherein R 7  is C 1 -C 4  alkyl;      by reacting with additional BCl 3 ;    (c) quenching the reaction of step (b) with methanol; and    (d) isolating the crystalline solvate.    
     
     
         54 . The process of  claim 53  wherein the organic solvent is 1,2-dichloroethane.  
     
     
         55 . The process of  claim 53  wherein R 4  is methoxy, and R 5  and R 7  are methyl.  
     
     
         56 . A process for preparing the crystalline solvate of  claim 33 , comprising the steps of: 
 (a) acylating a benzothiophene of the formula                          wherein: 
 R 4  is C 1 -C 4  alkoxy and R 5  is C 1 -C 4  alkyl, with an acylating agent of the formula  
                     
   wherein: 
 R 6  is chloro, and R 2  and R 3  together with the adjacent nitrogen atom form a piperidino group, and HX is HCl, in the presence of BCl 3  in 1,2-dichloroethane;  
   (b) dealkylating the hydrochloride salt of the compound of the formula                        wherein R 7  is C 1 -C 4  alkyl;      by reacting with additional BCl 3 ;    (c) quenching the reaction of step (b) with ethanol; and    (d) isolating the crystalline solvate.    
     
     
         57 . The process of  claim 56  wherein R 4  is methoxy, and R 5  and R 7  are methyl.  
     
     
         58 . A process for preparing a crystalline solvate of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride having the following X-ray diffraction pattern obtained with copper radiation:  
       
         
           
                 
                 
                 
               
                     
                     
                 
                     
                     
                 
                     
                   d-line spacing 
                   I/I o   
                 
                     
                   (Angstroms) 
                   (x100) 
                 
                     
                     
                 
                     
                 
                 
                 
                 
               
                     
                   14.3518 
                   7.24 
                 
                     
                   10.3335 
                   6.17 
                 
                     
                   8.8305 
                   4.29 
                 
                     
                   7.9475 
                   38.16 
                 
                     
                   6.5904 
                   64.25 
                 
                     
                   6.2848 
                   6.52 
                 
                     
                   5.6048 
                   28.06 
                 
                     
                   5.4107 
                   100.00 
                 
                     
                   5.1544 
                   11.26 
                 
                     
                   5.0493 
                   53.26 
                 
                     
                   5.0224 
                   46.11 
                 
                     
                   4.8330 
                   76.94 
                 
                     
                   4.7694 
                   34.23 
                 
                     
                   4.6461 
                   50.22 
                 
                     
                   4.5754 
                   38.61 
                 
                     
                   4.4953 
                   72.65 
                 
                     
                   4.3531 
                   49.15 
                 
                     
                   4.2940 
                   41.64 
                 
                     
                   4.2425 
                   35.75 
                 
                     
                   4.1856 
                   21.63 
                 
                     
                   4.1338 
                   9.47 
                 
                     
                   4.0793 
                   12.69 
                 
                     
                   3.9960 
                   18.50 
                 
                     
                   3.9037 
                   9.03 
                 
                     
                   3.7854 
                   40.39 
                 
                     
                   3.7521 
                   54.16 
                 
                     
                   3.6787 
                   28.60 
                 
                     
                   3.6509 
                   17.96 
                 
                     
                   3.5444 
                   31.72 
                 
                     
                   3.4679 
                   41.55 
                 
                     
                   3.3899 
                   7.69 
                 
                     
                   3.3101 
                   5.72 
                 
                     
                   3.2561 
                   7.42 
                 
                     
                   3.1784 
                   15.19 
                 
                     
                   3.0445 
                   11.17 
                 
                     
                   3.0146 
                   8.94 
                 
                     
                   2.9160 
                   11.89 
                 
                     
                   2.8217 
                   18.23 
                 
                     
                   2.7500 
                   12.06 
                 
                     
                   2.6436 
                   9.65 
                 
                     
                   2.6156 
                   6.97 
                 
                     
                     
                 
                     
                     
                 
             
                
                
                
                
                
               
               
                
               
            
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
         comprising the steps of: 
 (a) acylating a benzothiophene of the formula  
                     
 
         wherein: 
 R 4  is C 1 -C 4  alkoxy and R 5  is C 1 -C 4  alkyl, with an acylating agent of the formula  
                     
 
         wherein: 
 R 6  is chloro, and R 2  and R 3  together with the adjacent nitrogen atom form a piperidino group, and HX is HCl, in the presence of BCl 3  in chlorobenzene;  
 
         (b) dealkylating the hydrochloride salt of the compound of the formula  
         
           
             
             
                 
                 
             
           
           wherein R 7  is C 1 -C 4  alkyl;  
         
         by reacting with additional BCl 3 ;  
         (c) quenching the reaction of step (b) with methanol; and  
         (d) isolating the crystalline solvate.  
       
     
     
         59 . The process of  claim 58  wherein R 4  is methoxy, and R 5  and R 7  are methyl.  
     
     
         60 . A process for preparing non-soLvated crystalline 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride comprising (a) reacting a solvated form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene hydrochloride in methanol or in a mixture of methanol and water with about one equivalent of base, 
 (b) extracting the solution from step (a) with an aliphatic hydrocarbon solvent,    (c) adding about one equivalent of hydrochloric acid to the methanolic solution from step (b), and    (d) isolating the crystalline compound.    
     
     
         61 . The process of  claim 60  wherein the aliphatic hydrocarbon solvent is hexane or heptane.  
     
     
         62 . The process of  claim 60  wherein the base is sodium hydroxide.  
     
     
         63 . The process of  claim 60  wherein the hydrochloric acid is a 2 N aqueous solution.  
     
     
         64 . A process for preparing non-solvated crystalline 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]-benzo[b]thiophene hydrochloride comprising 
 (a) reacting a solvated form of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene hydrochloride in methanol or in a mixture of methanol and water with about one equivalent of base, and    (b) adding about one equivalent of hydrochloric acid to the methanolic solution from step (a), and    (c) isolating the crystalline compound.    
     
     
         65 . The process of  claim 64  wherein the base is sodium hydroxide.  
     
     
         66 . The process of  claim 64  wherein the hydrochloric acid is a 2 N aqueous solution.  
     
     
         67 . Non-solvated crystalline 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene hydrochloride, having substantially the following X-ray diffraction pattern obtained with copper radiation:  
       
         
           
                 
                 
                 
               
                     
                     
                 
                     
                     
                 
                     
                   d-line spacing 
                   I/I o   
                 
                     
                   (Angstroms) 
                   (x100) 
                 
                     
                     
                 
                     
                 
                 
                 
                 
               
                     
                   13.3864 
                   71.31 
                 
                     
                   9.3598 
                   33.16 
                 
                     
                   8.4625 
                   2.08 
                 
                     
                   7.3888 
                   7.57 
                 
                     
                   6.9907 
                   5.80 
                 
                     
                   6.6346 
                   51.04 
                 
                     
                   6.1717 
                   29.57 
                 
                     
                   5.9975 
                   5.67 
                 
                     
                   5.9135 
                   9.87 
                 
                     
                   5.6467 
                   38.47 
                 
                     
                   5.4773 
                   10.54 
                 
                     
                   5.2994 
                   4.74 
                 
                     
                   4.8680 
                   4.03 
                 
                     
                   4.7910 
                   5.98 
                 
                     
                   4.6614 
                   57.50 
                 
                     
                   4.5052 
                   5.75 
                 
                     
                   4.3701 
                   9.03 
                 
                     
                   4.2516 
                   69.99 
                 
                     
                   4.2059 
                   57.64 
                 
                     
                   4.1740 
                   65.07 
                 
                     
                   4.0819 
                   12.44 
                 
                     
                   3.9673 
                   22.53 
                 
                     
                   3.9318 
                   100.00 
                 
                     
                   3.8775 
                   9.07 
                 
                     
                   3.7096 
                   33.38 
                 
                     
                   3.6561 
                   21.65 
                 
                     
                   3.5576 
                   3.36 
                 
                     
                   3.5037 
                   7.97 
                 
                     
                   3.4522 
                   18.02 
                 
                     
                   3.4138 
                   4.65 
                 
                     
                   3.2738 
                   10.23 
                 
                     
                   3.1857 
                   8.90 
                 
                     
                   3.1333 
                   6.24 
                 
                     
                   3.0831 
                   9.43 
                 
                     
                   3.0025 
                   12.13 
                 
                     
                   2.9437 
                   4.96 
                 
                     
                   2.8642 
                   7.70 
                 
                     
                   2.7904 
                   11.95 
                 
                     
                   2.7246 
                   3.05 
                 
                     
                   2.6652 
                   3.32 
                 
                     
                   2.5882 
                   7.30 
                 
                     
                     
                 
                     
                     
                 
             
                
                
                
                
                
               
               
                
               
            
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         68 . The crystalline 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene hydrochloride of  claim 67  wherein the amount of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene hydro-chloride present is at least 95% by weight.  
     
     
         69 . The crystalline 6-hydroxy-2-(4—hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene hydrochloride of  claim 68  substantially free from chlorobenzene.  
     
     
         70 . The crystalline 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene hydrochloride of  claim 69  substantially free from aluminum salts or organoaluminum impurities.  
     
     
         71 . The crystalline 6-hydroxy-2-(4—hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene hydrochloride of claim  70  substantially odor free.  
     
     
         72 . A pharmaceutical formulation comprising the crystalline compound of any one of claims  67  to 71 and one or more pharmaceutically-acceptable carriers, diluents, or excipients.  
     
     
         73 . Crystalline 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene hydrochloride when prepared by the process of  claim 60 .  
     
     
         74 . Crystalline 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene hydrochloride when prepared by the process of  claim 64 .  
     
     
         75 . A process for preparing a crystalline solvate of 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[b]thiophene hydrochloride having the following X-ray diffraction pattern obtained with copper radiation:  
       
         
           
                 
                 
                 
               
                     
                     
                 
                     
                     
                 
                     
                   d-line spacing 
                   I/I o   
                 
                     
                   (Angstroms) 
                   (x100) 
                 
                     
                     
                 
                     
                 
                 
                 
                 
               
                     
                   10.3696 
                   14.40 
                 
                     
                   8.9032 
                   10.19 
                 
                     
                   8.3125 
                   7.61 
                 
                     
                   7.9818 
                   41.03 
                 
                     
                   7.2036 
                   7.34 
                 
                     
                   6.5411 
                   74.18 
                 
                     
                   6.2367 
                   6.39 
                 
                     
                   5.5539 
                   20.11 
                 
                     
                   5.3689 
                   100.00 
                 
                     
                   5.0272 
                   95.92 
                 
                     
                   4.7085 
                   89.13 
                 
                     
                   4.6406 
                   73.37 
                 
                     
                   4.6199 
                   77.58 
                 
                     
                   4.5347 
                   69.70 
                 
                     
                   4.4818 
                   49.86 
                 
                     
                   4.2589 
                   47.69 
                 
                     
                   4.2067 
                   44.43 
                 
                     
                   4.1659 
                   44.16 
                 
                     
                   4.0957 
                   11.96 
                 
                     
                   3.9347 
                   11.28 
                 
                     
                   3.7818 
                   40.90 
                 
                     
                   3.7614 
                   53.53 
                 
                     
                   3.6375 
                   36.68 
                 
                     
                   3.5773 
                   20.11 
                 
                     
                   3.5037 
                   25.14 
                 
                     
                   3.4409 
                   32.34 
                 
                     
                   3.4270 
                   39.54 
                 
                     
                   3.3088 
                   12.64 
                 
                     
                   3.2611 
                   9.65 
                 
                     
                   3.1046 
                   12.77 
                 
                     
                   3.0263 
                   17.53 
                 
                     
                   2.8536 
                   8.29 
                 
                     
                   2.8131 
                   12.09 
                 
                     
                   2.7309 
                   8.97 
                 
                     
                     
                 
                     
                     
                 
             
                
                
                
                
                
               
               
                
               
            
             
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
         comprising the steps of: 
 (a) dealkylating the hydrochloride salt of a compound of the formula  
                     
 wherein R 7  is C 1 -C 4  alkyl,  
 by reacting with BCl 3  in chloroform or methylene chloride;  
 (b) quenching the reaction of step (a) with methanol, ethanol, or i-propanol; and  
 (c) isolating the crystalline solvate.  
 
       
     
     
         76 . The process of claim  75  wherein R 7  is methyl.

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