Gong Liu-Zhu, Chen Xiao-Hua, Xu Xiao-Ying
Hefei National Laboratory for Physical Sciences at the Microscale, Department of Chemistry, University of Science and Technology of China, Hefei, 230026, China.
Chemistry. 2007;13(32):8920-6. doi: 10.1002/chem.200700840.
The Biginelli reaction, known for over 100 years, is an important multicomponent reaction for accessing dihydropyrimidinones (DHPMs). The individual enantiomers of DHPMs exhibit different or even opposite pharmaceutical activities, which require synthetic methods to easily access the optically pure DHPMs. In recent decades, many efforts have focused on developing procedures for the preparation of optically active Biginelli products. In this article, we will summarize the developments in the synthetic methods to access optically active DHPMs with an emphasis on the recent advances in the asymmetric catalytic Biginelli reactions, along with concepts to design the organocatalytic asymmetric variants.
比吉内利反应已有100多年的历史，是合成二氢嘧啶酮（DHPMs）的重要多组分反应。DHPMs的各个对映体表现出不同甚至相反的药理活性，这就需要有能够轻松获得光学纯DHPMs的合成方法。近几十年来，许多工作都集中在开发制备光学活性比吉内利产物的方法上。在本文中，我们将总结合成光学活性DHPMs的方法进展，重点介绍不对称催化比吉内利反应的最新进展，以及设计有机催化不对称变体的概念。
