一种用于手性 α-杂环化合物对映选择性合成的通用方法。

A general method for the enantioselective synthesis of α-chiral heterocycles.

机构信息

Department of Chemistry, University of Houston, 136 Fleming Building, Houston, Texas 77204-5003, USA.

出版信息

Org Lett. 2012 Dec 7;14(23):6104-7. doi: 10.1021/ol3030605. Epub 2012 Nov 16.

Abstract

The enantioselective formation of stereocenters proximal to unprotected heterocycles has been accomplished. Thus, vinyl boronic acids are added to heterocycle-appended enones via a modified-BINOL catalyst. Catalyst design was key to enable a general reaction. High yields and useful er's are observed for a host of common heteroaryls.

摘要

已实现了非保护杂环附近立体中心的对映选择性形成。因此，通过修饰的联萘酚催化剂将乙烯基硼酸添加到杂环取代的烯酮中。催化剂设计是实现通用反应的关键。观察到许多常见杂芳基的高收率和有用的对映选择性。