Synthesis Process Aromatase Inhibitors Anastrozole

The pathogenesis of breast cancer and present situation of the treatment for breast cancer were briefly reviewed in this paper. The action mechanism and clinic application of anastrozole were briefly reviewed in this thesis.The synthetic methods for anastrozole were investigated and an economical and reasonable synthetic route was studied. The target compound was synthesized with a total yield of 14.8％from 3, 5-dimethylbenzoic acid via esterification, bromination, cyanidation, methylation, reducetion, chlorination, N-alkylation and deamination. In the bromination step, carbon tetrachloride was replaced by methylene chloride, the yield was enhanced and the toxicity was reduced; The reactive time was shorten and the yield was enhanced by using alcohol-water as solvent in the cyanidation; The operation was easier and safer by using potassium hydroxide instead of sodium hydride in the methylation; Successfully using sodium borohydride and lithium chloride as reducing agent in the reduction, the cost was saved. The synthetic procedure of the intermediates was studied intensively and optimized. The operation was simplified and could be practical on a large scale. All the materials are available domestically.Anastrozole was identified by ~1H-NMR, MS and IR.