Study on synthesis of Gefitinib for cancer drug

Abstract

This paper reports a method for synthesis of Gefitinib starting from 3-hydroxy-4-methoxy benzaldehyde. Gefitinib is used for the treatment of non-small cell lung cancer (NSCLC), pancreatic cancer and other cancers. The process includes alkylation of starting material, conversion of aldehyde into the corresponding nitrile, nitration, reduction, cyclization and reaction with 3-chloro-4-fluoroaniline to afford Gefitinib with seven steps and overall productivity of 15.88%. The product and intermediates have been characterized by IR, 1 H-NMR, 13C-NMR, MS.