Synthesis Process Research Of Aromatase Inhibitors Letrozole

This article summarizes the mechanism in human’s body of aromatase inhibitors,and it’s development process, each generation of representative drugs, and the roleand status of aromatase inhibitors in estrogen dependent disease, such as breast cancer,endometriosis. The structure, naming, properties, pharmacokinetic and pharmacologic-al effects of letrozole, which are the nonsteroidal and the third generation aromataseinhibirors, was introduced.The synthetic methods for letrozole were investigated and an simple, feasible andeasy to industrialized production of synthetic route was studied: the target compoundwas synthesized with a total yield of15.6%from p-Tolunitrile and4-chlorobenzonitrile via three steps of reaction, i.e., subsititution reaction,bromination reaction and condensation reaction. For every step of the synthetic routeof the synthesis process were studied intensively, optimizing the reaction conditions.All the materials are available domestically, and the price is cheap. The syntheticroute is shorter, and don’t need through column chromatography purification, suitablefor industrial production.Letrozole structure and synthesis of intermediates were confirmed by1H-NMR,13C-NMR and FT-IR.