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

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.

SUBMITTER: Qin Y

PROVIDER: S-EPMC8148391 | biostudies-literature | 2019 Dec

REPOSITORIES: biostudies-literature

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

Qin Yuman Y Han Yujie Y Tang Yongzhen Y Wei Junfa J Yang Mingyu M

Chemical science 20191206 5

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 wa ...[more]

PMID: 34123252

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