对映纯3,4-二氢嘧啶酮衍生物的合成研究进展

Progress on the Synthesis of Enantiomerically Pure 3,4-Dihydropyrimidin-2-one Derivatives

3,4-二氢嘧啶酮本身是不对称分子,但绝大多数Biginelli反应得到的都是外消旋的3,4-二氢嘧啶酮类化合物.大量研究表明3,4-二氢嘧啶酮的C(4)立体中心的绝对构型对其生物活性有重要影响.主要归纳了获得对映纯3,4-二氢嘧啶酮类化合物的新发展,特别是不对称催化Biginelli反应合成此类化合物的文献方法.

3,4-Dihydropyrimidinethiones are chiral molecules, however, only racemic products are isolated in the most reported Biginelli reactions. It has been proved that the absolute configuration of the C（4） stereogenic center has significant influence on the biological activity. The development in the accessing of optically active 3,4-dihydropyrimidinethiones focusing on the recent advances in the asymmetric catalytic Biginelli reactions is summarized.