Improvement of the synthesis of gefitinib / 中国药学杂志

ABSTRACT

OBJECTIVE: To synthesize gefitinib. METHODS: Gefitinib was synthesized from vertraldethyde via nitration, hydrolysis, conversion of aldehyde to nitrile, condensation with N-(3-chloropropyl) morpholine, conversion of nitrile to amide, reduction, then cyclization to give 7-methoxy-6-(3-morpholinopropoxy) -3, 4-dihydroquinazolin-4-one, which was finally subjected to chlorination and condensation with 3-chloro-4-fluoroaniline. RESULTS: The chemical structure of the target compound was confirmed by MS, 1H-NMR and 13C-NMR. CONCLUSION: This article provides a novel and more reasonable process for the manufacturing of gefitinib.