| 摘要 |
<p>PROBLEM TO BE SOLVED: To provide an improved method for the synthesis of erlotinib (N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine) and its pharmaceutically acceptable salts.SOLUTION: A method comprises reacting a 4-halo-6,7-bis(2-methoxyethoxy) quinazoline with 3-aminophenyl acetylene or a salt thereof under acidic conditions where an acid is used which may be selected from the group consisting of hydrochloric acid, hydrobromic acid, sulfuric acid, p-toluene sulfonic acid, benzoic acid, citric acid, succinic acid, oxalic acid, benzene sulfonic acid, tartaric acid, methane sulfonic acid, phosphoric acid and mixtures thereof, thereby forming the corresponding acid salt of erlotinib shown in formula described below.</p> |
