Patent ID: 8609841
Filing Date: 2013-12-17
Classification: C07D

Abstract:
1. A method for the preparation of Erlotinib of formula (I) or a salt thereof: comprising the following steps: (a) Reaction of the 3-substituted aniline of formula (V-a): where X is selected from the group consisting in Iodine, Bromine, Chlorine, OTs, OMs, with 4-hydroxy-4-methyl-2-pentinoic acid of formula (V): to obtain 4-(3-aminophenyl)-2-methyl-3-butyn-2-ol of formula (IV): (b) Reaction of the intermediate (IV) with 4-chloro-6,7-bis(2-methoxyethoxy)quinazoline of formula (III) to obtain 3-Butyn-2-ol, 4-[3-[[6,7-bis(2-methoxyethoxy)-4-quinazolinyl]amine]phenyl]-2-methyl-, hydrochloride (1:1) of formula (II): (c) Conversion of the intermediate (II) to Erlotinib of formula (I); or a method wherein said steps (b) and (c) are replaced by the following steps: (d) conversion of the intermediate (IV) to 3-ethynylanyline of formula (IV-a): (e) Reaction of the intermediate of formula (IV-a) with 4-chloro-6,7-bis(2-methoxyethoxy)quinazoline of formula (III) to obtain Erlotinib of formula (I).