有机催化不对称Michael加成反应

Organocatalytic Asymmetric Michael Additions

有机催化的不对称合成反应是目前研究最为活跃的领域之一.不对称Michael加成反应是合成众多重要的手性合成子和药物中间体的有效手段.目前报道的催化Michael加成反应的有机催化剂主要有脯氨酸及其衍生物、手性咪唑啉酮、手性(硫)脲、金鸡纳碱衍生物等.对各类有机催化剂在有机催化不对称Michael加成反应中的应用,以及不对称诱导反应的机理、催化剂分子结构及反应条件对其催化活性和不对称诱导作用的影响进行了评述。

Organocatalytic asymmetric reaction is an increasingly active area in organic synthesis. The asymmetric Michael addition provides a rapid access to versatile important chiral building blocks and intermediates for the synthesis of bioactive agrochemicals and pharmaceutical compounds. The reported organocatalysts for asymmetric Michael additions include proline and its derivatives, chiral imidazolidinone derivatives, chiral （thio） urea, cinchona alkaloids and so on. The applications of various organocatalysts to asymmetric Michael additions are reviewed in this paper. The reaction mechanism, catalytic activity and the asymmetric induction influenced by the structure of organocatalysts and the reaction condition are also discussed.