A PROCESS FOR THE SYNTHESIS OF 6,7-BIS-(2-METHOXYETHOXY)-QUINAZOLIN-4-YL-(3-ETHYNYLPHENYL)AMINE HYDROCHLORIDE

摘要

The present invention provides a process for synthesizing [6,7 -bis(2- nethoxyethoxy)q u inazol i n-4-yl]-( 3-ethynylphenyl)amine hydrochloride Erlitinib Hydrochloride) having the formula comprising reacting 3,4-dihydroxy benzaldehyde with bromo derivative of ethyl methyl ether to obtain 3,4-bis(2-methoxyethoxy)-benzaldehyde having formula (III) . This is converted to give 3,4- bis (2- methoxyethoxy)-benzonitrile. On furthur nitration we obtain 4,5- bis (2- methoxyethoxy)-2-nitrobenzonitrile which on nitro reduction we get 2- amino-4,5-bis(2-methoxyethoxy)benzonitrile and reacting this with N"-(3- ethynylphenyl)-N,N-dimethyl formamidine gives erlotinib free base. On furthur treatment of this free base with methanolic/ethanolic hydrochloric acid gives us erlotinib hydrochloride.