Rh(III)-Catalyzed Synthesis of Amino-isocoumarins with N-Functionalized Cyclic Carbonates via C-H/O-H Annulation
Yuanfei Zhang1,2, Hao Wang1, Jintong Bai1
1Guangxi Key Laboratory of Natural Polymer Chemistry and Physics, Nanning Normal University, Nanning 530001, China.
Abstract:
A practical method to access amino-isocoumarins catalyzed by a Rh(III) complex through redox-neutral C-H/O-H annulation has been disclosed. The use of N-functionalized cyclic carbonates is crucial to facilitate the catalytic turnover, and a broad spectrum of amino-isocoumarin derivatives were prepared with satisfactory yields. Amino-isocoumarin estrone conjugated with a selenocyano functionality was identified to be nearly four times as active as the marketed drug abiraterone against T47D cancer cells.
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