4.7 Article

Rh(III)-Catalyzed C-H Cyanation of 2H-Indazole with N-Cyano-N-phenyl-p-toluenesulfonamide

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JOURNAL OF ORGANIC CHEMISTRY
卷 85, 期 16, 页码 10835-10845

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AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.0c01386

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  1. National Natural Science Foundation of China [21672192, 21803059, U1904212, 21929101]

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A Rh(III)-catalyzed direct cyanation of 2H-indazoles with N-cyano-N-phenyl-p-toluenesulfonamide has been realized via a chelation-assisted strategy. The methodology enables regioselective access to various ortho-cyanated phenylindazoles in good yields with a broad substrate scope and good functional group compatibility. The obtained cyanated indazoles could further be converted into other value-added chemicals. Importantly, the current protocol is featured with several characteristics, including a novel cyanating agent, good regioselectivity, and operational convenience.

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