title: Synthesis of gefitinib from methyl 3-hydroxy-4-methoxy-benzoate.
abstract: This paper reports a novel synthesis of gefitinib starting from methyl 3-hydroxy-4-methoxybenzoate. The process starts with alkylation of the starting material, followed by nitration, reduction, cyclization, chlorination and two successive amination reactions. The intermediates and target molecule were characterized by 1H-NMR, 13C-NMR, MS and the purities of all these compounds were determined by HPLC. This novel synthetic route produced overall yields as high as 37.4%.
authors.affiliation: Institute of Pharmaceutical Engineering, School of Chemistry and Chemical Engineering, Jiangsu Laboratory for Biomaterials and Devices, Southeast University, 210096 Nanjing, PR China. seu301@126.com
authors.forename: Ming Dong
authors.initials: MD
authors.lastname: Li
authors.forename: You Guang
authors.initials: YG
authors.lastname: Zheng
authors.forename: Min
authors.initials: M
authors.lastname: Ji
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry; D000077156:Gefitinib; D062385:Hydroxybenzoates / Q000737:chemistry*; D011799:Quinazolines / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D062385:Hydroxybenzoates; D011799:Quinazolines; D000077156:Gefitinib