铑（III）催化通过C-H/O-H环化反应合成带有官能化环状碳酸酯的氨基异香豆素。
Rh(III)-Catalyzed Synthesis of Amino-isocoumarins with -Functionalized Cyclic Carbonates via C-H/O-H Annulation.
作者信息
Zhang Yuanfei, Wang Hao, Bai Jintong, Liu Qiuxia, Cui Jianguo, Huang Yanmin
机构信息
Guangxi Key Laboratory of Natural Polymer Chemistry and Physics, Nanning Normal University, Nanning 530001, China.
State Key Laboratory of Structural Chemistry, Fujian Institute of Research on the Structure of Matter, Chinese Academy of Sciences, Fuzhou 350002, China.
出版信息
Org Lett. 2022 Dec 23;24(50):9222-9227. doi: 10.1021/acs.orglett.2c03739. Epub 2022 Dec 13.
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 -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.
已公开了一种通过氧化还原中性C-H/O-H环化反应，由铑（III）配合物催化制备氨基异香豆素的实用方法。使用官能化环状碳酸酯对于促进催化循环至关重要，并且制备了多种氨基异香豆素衍生物，产率令人满意。已确定与硒氰基官能团共轭的氨基异香豆素雌酮对T47D癌细胞的活性几乎是市售药物阿比特龙的四倍。
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