US2014194624A1PendingUtilityA1

Process for Preparation of Erlotinib and its Pharmaceutically Acceptable Salts

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Assignee: CIPLA LTDPriority: Apr 4, 2007Filed: Jan 13, 2014Published: Jul 10, 2014
Est. expiryApr 4, 2027(~0.7 yrs left)· nominal 20-yr term from priority
Inventors:Dharmaraj Ramachandra RaoRajendra Narayanrao Kankan
C07D 239/94A61P 43/00
59
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Claims

Abstract

A process for the preparation of a salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine comprising reacting a 4-halo-6,7-bis(2-methoxyethoxy)quinazoline with 3-aminophenyl acetylene or an acid salt thereof under acidic conditions to form the corresponding acid salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine, the process optionally further comprising converting the acid salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine to N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine.

Claims

exact text as granted — not AI-modified
1 . A sulphate salt, an oxalate salt, or a tosylate salt, or a succinate salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine prepared by a process comprising reacting a 4halo-6,7-bis(2-methoxyethoxy)quinazoline with 3-aminophenyl acetylene or an acid salt thereof under acidic conditions to form the corresponding acid salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin4-amine. 
     
     
         2 . The sulphate salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine of  claim 1 , wherein the acidic conditions are obtained using sulphuric acid. 
     
     
         3 . The oxalate salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine of  claim 1 , wherein the acidic conditions are obtained using, oxalic acid. 
     
     
         4 . The tosylate salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin4-amine of  claim 1 , wherein the acidic conditions are obtained using p-toluene sulphonic acid. 
     
     
         5 . The succinate salt of N-(3-ethynylphenyl)-6,7-bis(2.-methoxyethoxy)quinazolin4-amine of  claim 1 , wherein the acidic conditions are obtained using succinic acid. 
     
     
         6 . The sulphate salt, the oxalate salt, the tosylate salt, or the succinate salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine of  claim 1 , wherein the process further comprises converting the acid salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine to N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine. 
     
     
         7 . The sulphate salt, the oxalate salt, the tosylate salt, or the succinate salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine of  claim 1 , wherein the process further comprises basifying the acid salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine in the presence of a base to obtain N-(3-ethynylphenyl)-6,7-bis-methoxyethoxy)quinazolin-4-amine. 
     
     
         8 . The sulphate salt, the oxalate ash, the tosylate salt, or the succinate salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine of  claim 1 , wherein the process further comprises converting the N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine to the sulphate salt, the oxalate salt, the tosylate salt, or the succinate salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine. 
     
     
         9 . The sulphate salt, the oxalate salt, the tosylate salt, or the succinate salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin of  claim 1 , wherein the process is not carried out under an inert atmosphere. 
     
     
         10 . The sulphate salt the oxalate salt, the tosylate salt, or the succinate salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine of  claim 1 , wherein the process is carried out at a temperature below 40° C. 
     
     
         11 . The sulphate salt, the oxalate salt, the tosylate salt, or the succinate salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine of  claim 1 , wherein the process is carried out in the presence of a solvent selected from the group consisting of water, C 1 -C 4  alcohols, ketones, hydrocarbons or mixtures thereof. 
     
     
         12 . The sulphate salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxyl)quinazolin-4-amine of  claim 1 . 
     
     
         13 . The oxalate salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine of  claim 1 . 
     
     
         14 . The tosylate salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine of  claim 1 . 
     
     
         15 . The succinate salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine of  claim 1 . 
     
     
         16 . A sulphate salt, an oxalate salt, a tosylate salt, or a succinate salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine. 
     
     
         17 . The sulphate salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine of  claim 16 . 
     
     
         18 . The oxalate salt of 3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine of  claim 16 . 
     
     
         19 . The tosylate salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine of  claim 16 . 
     
     
         20 . The succinate salt of N-(3-ethynylphenyl)-6,7-bis(-methoxyethoxy)quinazolin-4-amine of  claim 16 .

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