Targeted Cancer Raw Material Drug Gefitinib Nepalese Synthesis And Process Optimization

Gifitinib is a kind of new molecular targeted cancer drugs which is a kind of tyrosine kinase inhibitor of epidermal growth factor receptor. It inhibits the growth of tumors by blocking tyrosine kinase signaling pathways.After analysing the synthetic routes which have been reported, we choose the fourth synthetic route to optimize synthetic process of Gefitinib, which 2-Amino-4, 5-dimethoxybenzoic acid was cyclized, monodemethylated, acetylated, chlorinated, ammoniated and alkylated to obtain the target compound. We improve the yield and purity of intermediates 6-hydroxy-7-methoxy-3,4-dihydroquinazolin-4-one and 4-[(3-Chlor-4-fluorophenyl)amino]-7-methoxyquinazolin-6-ol. Gefitinib is prepared in the total yield 19% and purity 99.5%.Gefitinib and its intermediates were confirmed by MS, IR,1HNMR,13CNMR, HPLC and melting point.