Development of chiral organo catalysts in which different atoms cooperatively catalyze asymmetric reactions

开发了一种新型的不对称有机催化剂，用于制备光学活性醇衍生物。该催化剂是一种亚膦酸衍生物，很容易从氨基吲哚衍生而来，其两个对映体都可以在商业上获得。特别是1，2-二醇在有机催化剂催化下的不对称去对称化反应，得到了具有高对映选择性和高产率的手性醇衍生物。此外，对环己基苯甲醇等外消旋醇类化合物也实现了高拆分效率的动力学拆分。

A novel asymmetric organocatalyst for preparation of optically active alcohol derivatives has been developed. The catalyst is a phosphinite derivative easily derived from aminoindanol whose both enantiomers are commercially available. Especially, asymmetric desymmetrization of 1, 2-diols by use of acylation reaction catalyzed by the organocatalyst gave desired chiral alcohol derivatives with high enantioselectivity and in high yield. In addition, kinetic resolution of racemic alcohols such as cyclohexylbenzyl alcohol was achieved with high level of resolution efficiency.