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本文报道了从表雄酮(从剑麻皂甙元制得的中间体)经6步反应制备抗心律失常新药安律酮(3α-氨基-2β-羟基-5α-雄甾烷-17酮盐酸盐)的合成方法,并改进了反应的部份条件,。在用钯/碳催化氢化叠氮化合物(Ⅵ)制备安律酮时,获得熔点为199°-201℃的副产物(Ⅸ),其结构经波谱与化学方法确证为3α-氯-2β-羟基-5α-雄甾烷-17酮。
This article reports the preparation of anti-arrhythmic drug regimen of ketanserin (3α-amino-2β-hydroxy-5α-androstane-17one hydrochloride Salt) synthesis method, and to improve the reaction conditions. The by-product (IX) having a melting point of 199 ° -201 ° C was obtained in the preparation of antlone by catalytic hydrogenation of the azido compound (VI) with palladium on carbon. The structure was confirmed by spectroscopy and chemical methods to be 3α-chloro-2β- -5 [alpha] -androstane-17one.