文献类型：期刊文献

中文题名：非那雄胺的合成

英文题名：Synthesis of finasteride

作者：杨艳[1];马红梅[2];屈战果[1];金永生[1];胡宏岗[1];吴秋业[1]

机构：[1]第二军医大学药学院有机化学教研室,上海200433;[2]华东理工大学药学院,上海200237

年份：2007

卷号：25

期号：5

起止页码：310

中文期刊名：药学实践杂志

外文期刊名：Journal of Pharmaceutical Practice

收录：CSTPCD

语种：中文

中文关键词：非那雄胺;孕烯醇酮醋酸酯;合成

外文关键词：finasteride ;pregnenolone acetic ester; synthesis

摘要：目的:非那雄胺的合成方法研究。方法:以孕烯醇酮醋酸酯为原料,经次溴酸钠氧化、甲醇甲酯化得到3-羰基-4-雄甾烯-17β-羧酸甲酯,再经Oppenauer氧化、双键的氧化切断、氨解环合、△5双键加氢、1,2位脱氢、Bodroux反应等8步反应制得非那雄胺。结果:总收率36.5%,可大大降低生产成本。结论:此方法原料易得、操作简单、成本低廉、收率高。
Objective ：To study the synthesis of finasteride. Methods： Finasteride was synthesized from pregnenolone acetic ester, and by hypobromous acid oxidation, methanol esterification to give 3-oxo-4-androstene-17β-carboxylic methyl ester. Then by Oppenauer oxidation,cleavage of Δ^4-dOuble bond by oxidation, ring closure by ammonia,hydrogenation of Δ^5-double bond, dehydrogenation of 1,2-position in A-ring and Bodroux reaction to get product. Results ： Overall yield was 36.5%. Conclusion ：The material of this synthesis is inexpensive, the process is simple, the cost is low and the yield is good