PROCESS FOR PREPARATION OF ERLOTINIB AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS

摘要

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.