一种非奈利酮消旋体的制备方法

A method for preparing a racemate of finerenone

摘要:

使用4-氰基-3-甲氧基苯甲醛和乙酰乙酸叔丁酯为原料通过缩合、关环、氧烷基化、水解以及氨解得到非奈利酮消旋体，该路线突破了常规酯难以水解的困难。对反应条件进行了一系列优化，放大到百克级最终以33.5%的总收率得到非奈利酮消旋体，结果表明该路线反应条件温和，收率高，为合成非奈利酮原料药提供了一条合理的路线。产物经 1 HNMR、13CNMR 和 HRMS 进行了结构确定。

Abstract:

Using 4-cyano-3-methoxybenzaldehyde and tert-butyl acetoacetate as raw materials, finerenone racemes were obtained through condensation, cyclization, oxyalkylation, hydrolysis and ammonolysis, which broke through the difficulty of hydrolysis of conventional esters. A series of optimization of reaction conditions were carried out, and the finerenone racemes were obtained with a total yield of 33.5%. The results showed that the reaction conditions were mild and the yield was high, which provided a reasonable route for the synthesis of finerenone raw materials. The structure of the product was determined by 1 HNMR, 13CNMR and HRMS.