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Org Lett. 2016 Aug 5;18(15):3898-901. doi: 10.1021/acs.orglett.6b01916. Epub 2016 Jul 21.

Selective Synthesis of Isoquinolines by Rhodium(III)-Catalyzed C-H/N-H Functionalization with α-Substituted Ketones.

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School of Pharmaceutical Sciences, Jiangnan University , Lihu Road 1800, 214122 Wuxi, P. R. China.


A rhodium(III)-catalyzed C-H/N-H bond functionalization for the synthesis of 1-aminoisoquinolines from aryl amidines and α-MsO/TsO/Cl ketones was achieved under mild reaction conditions. Thus, this approach provides a practical method for the site-selective synthesis of various synthetically valuable isoquinolines with wide functional group tolerance.

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