US2008221349A1PendingUtilityA1

Preparation of Amides of Retinoic Acid Via Mixed Anhydride and Mixed Carbonate Intermediates

50
Individually held — no corporate assignee on recordPriority: Mar 8, 2007Filed: Jan 2, 2008Published: Sep 11, 2008
Est. expiryMar 8, 2027(~0.6 yrs left)· nominal 20-yr term from priority
Inventors:John E. CabajJeff HutchisonJames Robert Zeller
C07C 231/02C07C 2601/16
50
PatentIndex Score
0
Cited by
0
References
0
Claims

Abstract

Processes for preparing amides of retinoic acid are disclosed. Intermediates useful in the preparation of amides of retinoic acid are also disclosed. In one version of the invention, fenretinide is produced via activation of retinoic acid (tretinoin) via its corresponding mixed anhydride or mixed carbonate followed by reaction of the activated intermediate with 4-aminophenol. Other amides of retinoic acid and isomers of retinoic acid, such as the 9-cis-form or 13-cis-form can also be made by this invention.

Claims

exact text as granted — not AI-modified
1 . A compound having the formula: 
       
         
           
           
               
               
           
         
       
       or isomers thereof, wherein R is alkyl or aryl or alkoxy with the proviso that R is not tertiary butyl. 
     
     
         2 . The compound of  claim 1  wherein:
 R is trimethylalkyl.   
     
     
         3 . The compound of  claim 1  wherein:
 R is —C(CH 3 ) 2 CH 2 CH 3 .   
     
     
         4 . The compound of  claim 1  wherein:
 R is —OCH 2 CH(CH 3 ) 2 .   
     
     
         5 . The compound of  claim 1  wherein:
 R is —OCH(CH 3 ) 2 .   
     
     
         6 . The compound of  claim 1  wherein:
 the compound is in all-trans form.   
     
     
         7 . The compound of  claim 1  wherein:
 the compound is in 9-cis form.   
     
     
         8 . The compound of  claim 1  wherein:
 the compound is in 13-cis form.   
     
     
         9 . The compound of  claim 1  wherein:
 R is straight chain alkyl.   
     
     
         10 . The compound of  claim 1  wherein:
 R is branched alkyl.   
     
     
         11 . The compound of  claim 1  wherein:
 R is substituted alkyl.   
     
     
         12 . The compound of  claim 1  wherein:
 R is unsubstituted alkyl.   
     
     
         13 . The compound of  claim 1  wherein:
 R is straight chain alkoxy.   
     
     
         14 . The compound of  claim 1  wherein:
 R is branched alkoxy.   
     
     
         15 . The compound of  claim 1  wherein:
 R is substituted alkoxy.   
     
     
         16 . The compound of  claim 1  wherein:
 R is unsubstituted alkoxy.   
     
     
         17 . The compound of  claim 1  wherein:
 R is substituted aryl.   
     
     
         18 . The compound of  claim 1  wherein:
 R is unsubstituted aryl.

Join the waitlist — get patent alerts

Track US2008221349A1 — get alerts on status changes and closely related new filings.

We store only your email — no account needed. See our privacy policy.