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
出处
《药学实践杂志》
CAS
2007年第5期310-312,共3页
Journal of Pharmaceutical Practice
关键词
非那雄胺
孕烯醇酮醋酸酯
合成
finasteride
pregnenolone acetic ester
synthesis
作者简介
杨艳（1971-），女，助理研究员，主要从事新药研究与开发．Tel：13585871896
通讯作者：吴秋业（1964-），Tel：（021）25070381，E-mail：Wuqysmmu@sohu．com
