剑麻皂甙元资源利用的研究Ⅱ.抗心律失常药安律酮的合成
The Utilization of Tigogenin Ⅱ.Synthesis of Auluton -- An Antiarrhythmic Agent
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摘要: 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。Abstract: This paper describes a method of synthesis of a new anti-arrhythmie agent-Au1uton( V Ⅱ.3α-amin-2β-hydroxy-5α-androstan-17-one hvdrochloride ), prepared fromepiandrosterone (an intermediate - derived from tigogenin) by a six-step process. Some reaction conditions have been modified.When Auluton is made from the azido compound(VI) by pd/c catalytic hydrogenation.a by-product (IX mp 199-201℃) has been obtained. Its structure is identified to be 3α-ch1oro-2β-hydorxy-5α-androstan-17-one by chemical and spectral data.
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Keywords:
- Antiarrhythmic agent /
- Amino steroid /
- Tigogenin
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