Improved synthesis of leonurine as cardioprotective agent

益母草碱作为一种具有心血管系统保护作用的天然产物的合成研究(英文)

A new synthetic method of leonurine was developed. Leonurine 1 was synthesized from the key intermediates 4 and 5, two compounds with high solubility in dichloromethane which allowed the synthetic procedure to be performed under mild conditions and afforded 1 with a good yield. Comparing the previous methods, the yield was increased from 30% to 54%, time consumed was significantly reduced as well.

本文报道了益母草碱合成新方法。用化合物4和5作为关键中间体, 在合成的过程中, 由于这两种化合物在有机溶剂中具有较好的溶解性, 使得关键缩合反应可以在较温和的反应条件下进行, 最终以较好的产率得到目标化合物益母草碱。与已报道的益母草碱合成方法相比, 合成产率由30%升至54%, 反应时间也大大缩短。