State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, 38 Xueyuan Road, Beijing, 100191, P. R. China.
Chem Commun (Camb). 2010 Mar 28;46(12):2124-6. doi: 10.1039/b923925a. Epub 2010 Feb 19.
The first direct organocatalytic asymmetric vinylogous Michael addition reactions of gamma-butenolides to chalcones have been developed by using chiral 1,2-diaminocyclohexane as a novel organocatalyst via a di-iminium transition state to provide syn-Michael products with good yields, high diastereoselectivities and enantioselectivities (up to 78% yield, >99 : 1 dr and 96% ee).
首次发展了一类新型手性 1,2-二氨基环己烷有机小分子催化剂，通过双亚胺过渡态实现了γ-丁内酯与查耳酮的首例直接不对称烯醇式迈克尔加成反应，以中等到优秀的收率（高达 78%）、极好的对映选择性（高达 96%ee）和非对映选择性（>99:1 dr），获得了 syn-Michael 加成产物。
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