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通过可裂解导向基团实现钯催化的未活化C(sp)-H键的分子间胺化反应。

Palladium-catalyzed intermolecular amination of unactivated C(sp)-H bonds via a cleavable directing group.

作者信息

Jin Lianwen, Zeng Xiaoli, Li Siyang, Hong Xuechuan, Qiu Guofu, Liu Peng

机构信息

Ministry of Education Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, School of Pharmaceutical Sciences, Wuhan University, Wuhan, 430071, China.

出版信息

Chem Commun (Camb). 2017 Apr 4;53(28):3986-3989. doi: 10.1039/c7cc00808b.

Abstract

Palladium-catalyzed intermolecular amination of unactivated C(sp)-H bonds was developed. Using NFSI as both the amino source and the oxidant, this protocol operates under mild conditions with excellent terminal selectivity and a broad substrate scope. Moreover, the directing group can be easily removed to produce 1,2-amino alcohols.

摘要

开发了钯催化的未活化C(sp)-H键的分子间胺化反应。使用NFSI作为氨基源和氧化剂,该方法在温和条件下进行,具有出色的末端选择性和广泛的底物范围。此外,导向基团可以很容易地除去以生成1,2-氨基醇。

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