Process for preparation of erlotinib and its...

Details Process for preparation of erlotinib and its... Process for preparation of erlotinib and its...

C - Chemistry, Metallurgy

07

D

C07D 239/94 (2006.01)

Patent

CA 2682013

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.

Cette invention a trait à un procédé de préparation d'un sel de la N-(3-éthynylphényl)-6,7-bis(2- méthoxyéthoxy)quinazolin-4-amine comprenant la mise en réaction d'une 4~halogéno-6,7-bis(2-méthoxyéthoxy) quinazoline avec de l'acétylène 3-aminophényle ou avec l'un de ses sels acides dans des conditions acides de manière à former le sel acide correspondant de la N-(3-éthynylphényl)-6,7-bis(2-méthoxyéthoxy)quinazolin-4-amine, ledit procédé comprenant par ailleurs éventuellement la conversion du sel acide de la N-(3-éthynylphényl)-6,7-bis(2-méthoxyéthoxy)quinazolin-4-amine en N-(3-éthynylphényl)-6,7-bis(2-méthoxyéthoxy)quinazolin-4-amine.

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