手性伯胺硫脲盐催化的α,α-二取代醛与马来酰亚胺的高效不对称迈克尔加成反应。
A highly efficient asymmetric Michael addition of α,α-disubstituted aldehydes to maleimides catalyzed by primary amine thiourea salt.
机构信息
Engineering Research Centre of Pharmaceutical Process Chemistry, Ministry of Education, School of Pharmacy, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, China.
出版信息
Org Biomol Chem. 2010 Oct 21;8(20):4767-74. doi: 10.1039/c0ob00154f. Epub 2010 Aug 23.
PMID:20730207
Abstract
The first highly efficient Michael addition of challenging α,α-disubstituted aldehydes to maleimides catalyzed by a simple bifunctional primary amine thiourea catalyst/benzoic acid system has been successfully developed to generate quaternary carbon centers in high yields (up to 99%) with excellent enantioselectivities (91-99%).
摘要
一种简单的双功能伯胺硫脲催化剂/苯甲酸体系，成功地实现了首例高效迈克尔加成反应，用于催化具有挑战性的α,α-二取代醛与马来酰亚胺的加成反应，以高产率（高达 99%）和优异的对映选择性（91-99%）生成季碳中心。
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