Laboratoire de Pharmaco-Chimie Radicalaire, Faculté de Pharmacie, Institut de Chimie Radicalaire ICR, UMR 7273, Aix-Marseille Univ, CNRS, 27 Bd Jean Moulin, CS 30064, 13385 Marseille Cedex 05, France.
Molecules. 2012 Apr 10;17(4):4313-25. doi: 10.3390/molecules17044313.
A three step synthesis of various thiobarbiturate derivatives 17-24 was established. The first step is mediated by Mn(OAc)₃, in order to generate a carbon-carbon bond between a terminal alkene and malonate. Derivatives 1-8 were obtained in moderate to good yields under mild conditions. This key step allows synthesis of a wide variety of lipophilic thiobarbiturates, which could be tested for their anticonvulsive or anesthesic potential.
建立了一个三步合成各种硫代巴比妥酸衍生物 17-24 的方法。第一步是由 Mn(OAc)₃介导的,目的是在末端烯烃和丙二酸酯之间生成碳-碳键。在温和条件下,以中等至良好的收率得到了衍生物 1-8。这个关键步骤允许合成各种亲脂性硫代巴比妥酸,这些化合物可以测试其抗惊厥或麻醉的潜力。