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对羟基苯甲酸甲酯经硝化、还原、乙酰化及醚化制得3-乙酰胺基-4-乙氧基苯甲酸甲酯(7),7再经硝化、还原、缩合、环合、氯代等反应制得关键中间体3-氰基-4-氯-6-乙酰胺基-7-乙氧基喹啉(12),12与3-氯-4-(吡啶-2-甲氧基)苯胺缩合并脱去乙酰基后再和4-二甲胺基巴豆酰氯反应制得来那替尼,总收率约29%。
Methyl p-hydroxybenzoate is prepared by nitration, reduction, acetylation and etherification of methyl 3-acetamido-4-ethoxybenzoate (7) followed by nitration, reduction, condensation, cyclization, Generation of the key intermediate 3-cyano-4-chloro-6-acetamido-7-ethoxyquinoline (12) ) Aniline condensation and deacetylation acetyl and then 4-dimethylaminocrotonic acid chloride reaction to prepare the system, the total yield of about 29%.