抗心律失常药安律酮衍生物的合成

SYNTHESIS OF THE DERIVATIVES OF AULUTON AN ANTIARRHYTHMIC AGENT

摘要: 本文报道4类抗心律失常药安律酮衍生物的合成。以安律酮碱(Ⅵ)与相应的酰氯反应制得 N-酰化衍生物(Ⅶa-d);2β-羟基-3α-叠氮基-5α-雄甾烷-17-酮(Ⅴ)用相应的酰氯酯化得中间体(Ⅷa-c),经催化氢化、氯化氢成盐而得O-酰化衍生物(Ⅸa-c);将 O-酰化衍生物进一步酰化或 N-酰化衍生物进一步酯化制得 N-、O-双酰化衍生物(Xa-b);2β、3β-环氧-5α-雄甾烷-17-酮经相应的伯胺反应制得 N-烷基取代衍生物(Ⅺa-b)
- 剑麻皂甙元 /
- 安律酮衍生物 /
- 抗心律失常 /
- 5α-雄甾烷-17-酮
Abstract: This paper deals with the synthesis of Auluton-3α-amino-2β-hydroxy-5α-androstan-17-one hydrochloride, together with its 14 new derivatives: N—acyl derivatives(Ⅶ_a-b), O-acyl derivatives (Ⅸa-c), N- and O- diacyl derivatives(Xa-b), N-alkyl derivatives(Ⅺa-b) and 3 intermediates (Ⅷa-c). The structures of these new ccmpounds were confirmed on the basis of their spectral data and elementry analysis.
- Derivatives of Auluton /
- Antiarrhythmic agent.