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A general method for site-selective Csp3–S bond formation via cooperative catalysis

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Abstract

Herein, we report a copper-catalysed site-selective thiolation of Csp3–H bonds of aliphatic amines. The method features a broad substrate scope and good functional group compatibility. Primary, secondary, and tertiary C–H bonds can be converted into C–S bonds with a high efficiency. The late-stage modification of biologically active compounds by this method was also demonstrated. Furthermore, the one-pot preparation of pyrrolidine or piperidine compounds via a domino process was achieved.

Graphical abstract: A general method for site-selective Csp3–S bond formation via cooperative catalysis

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Article information


Submitted
21 Aug 2019
Accepted
05 Dec 2019
First published
06 Dec 2019

This article is Open Access
All publication charges for this article have been paid for by the Royal Society of Chemistry

Chem. Sci., 2020, Advance Article
Article type
Edge Article

A general method for site-selective Csp3–S bond formation via cooperative catalysis

Y. Qin, Y. Han, Y. Tang, J. Wei and M. Yang, Chem. Sci., 2020, Advance Article , DOI: 10.1039/C9SC04169A

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