依普利酮中间体坎利酮的合成工艺改进

Improved synthesis of canrenone, the intermediate of eplerenone

目的改进依普利酮中间体坎利酮的合成工艺。方法以去氢表雄酮为起始原料,经过氧化、烯醇醚化、环氧化、环缩合、脱羧和脱氢等6步反应合成坎利酮。结果合成了目标化合物坎利酮,其结构经IR、1H-NMR、13C-NMR和FAB-MS等方法确证。总收率为57·9%。结论与文献报道的工艺相比,改进后的工艺更为安全简便、步骤较少且收率较高。

Aim To synthesize canrenone, the intermediate of eplerenone and improve its synthetic process. Method Canrenone was synthesized from dehydroepiandrosterone by oxidation, enol etherification, oxirane formation, cyclocondensation, decarboxylation and dehydrogenation. Result The target compound was obtained and identified by IR, ^1H-NMR, ^13C-NMR and FAB-MS. The total yield was 57.9%. Conclusion Compared with the literature process, the improved process is secure, convenient and with higher-yield.