Patent ID: 8642758
Filing Date: 2014-02-04
Classification: A61P,C07D

Abstract:
1. A process for the preparation of an acid 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, wherein the process is carried out in the presence of a solvent selected from the group consisting of water, dimethyl carbonate, special denatured spirit (SPDS), acetonitrile, acetone, ethyl acetate, isopropyl alcohol and mixtures thereof, wherein the preparation of an acid salt of N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine is carried out at a temperature below 40° C.