论文部分内容阅读
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-3∝-叠氮基-5∝-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-5∝-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)
This article reports the synthesis of four antiarrhythmic drugs, anthrone derivatives. N-acylated derivatives (VIIa-d); 2β-hydroxy-3α-azido-5α-androstane-17-one (V (VIIIa-c) is esterified with the corresponding acid chloride to give O-acylated derivatives (IXa-c) by catalytic hydrogenation to form salts with hydrogen chloride; further acylation of the O-acylated derivatives or N- Acylation of derivatives further esterification to obtain N-, O-bis-acylated derivatives (Xa-b); 2β, 3β-epoxy-5α-Androstane-17-ketone by the corresponding primary amine reaction N-alkyl substituted derivatives (XIa-b)