沈阳药科大学学报

2008, No.148(05) 367-369

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阿那曲唑合成工艺改进
Improved synthetic procedure of anastrozole

匡金海,刘巍,周欣,董金华
KUANG Jin-hai,LIU Wei,ZHOU Xin,DONG Jin-hua(School of Pharmaceutical Engineering

摘要(Abstract):

目的改进芳香化酶抑制剂阿那曲唑的合成工艺。方法以3,5-二甲基苯甲酸为起始原料,经过酯化、溴化、氰化、甲基化、还原、氯代、N-烷基化和去氨基化合成阿那曲唑。结果产物结构经1H-NMR和MS确证。八步反应的总收率为24.2%。结论改进后的合成方法操作简便,适合工业化生产。
Objective To improve the synthetic procedure of aromatase inhibitor-anastrozole.Methods Using 3,5-dimethylbenzoic acid as the starting material,anastrozole was obtained via eight reaction steps,including esterification,bromination,cyanidation,methylation,reduction,chlorination,N-alkylation and deamination.Results The total yield was 24.2%.The structure of final product was confirmed by the analysis of 1H-NMR and MS.Conclusions Compared with the patent method,the improved process is convenient to operate with lower cost and higher yield and is more suitable for the production in large scale.

关键词(KeyWords): 制备;化学合成;阿那曲唑;芳香化酶抑制剂
preparation;chemical synthesis;anastrozole;aromatase inhibitor

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作者(Author): 匡金海,刘巍,周欣,董金华
KUANG Jin-hai,LIU Wei,ZHOU Xin,DONG Jin-hua(School of Pharmaceutical Engineering

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