非那雄胺的合成
Synthesis of finasteride
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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、v5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。Abstract: 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 △4-double bond by oxidation,ring closure by ammonia,hydrogenation of △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.
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Key words:
- finasteride /
- pregnenolone acetic ester /
- synthesis
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