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通过 N-单取代腙与烯酮的共轭加成反应催化不对称构建手性氢化哒嗪。

Catalytic asymmetric construction of chiral hydropyridazines via conjugate addition of N-monosubstituted hydrazones to enones.

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 Lett. 2013 Sep 6;15(17):4524-7. doi: 10.1021/ol4020865. Epub 2013 Aug 21.

Abstract

The first example of a highly enantioselective and scalable formal diaza-ene reaction between N-monosubstituted hydrazones and enones catalyzed by a simple chiral primary-second diamine salt has been developed. The catalytic process provides a highly practical and stereoselective synthetic method for chiral hydropyridazines.

摘要

首次发展了一种简单的手性伯胺仲二胺盐催化的 N-单取代腙和烯酮之间的高对映选择性和可规模化的形式氮杂-ene 反应。该催化过程为手性氢化吡啶嗪提供了一种高度实用和立体选择性的合成方法。

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