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Rh(iii)-catalyzed synthesis of tetracyclic isoquinolinium salts via C–H activation and [4+2] annulation of 1-phenyl-3,4-dihydroisoquinolines and alkynes in ethanol
Authors:Xinxin Dang  Yu He  Yingtian Liu  Xuehong Chen  Jun-Long Li  Xian-Li Zhou  Hezhong Jiang  Jiahong Li
Affiliation:School of Life Science and Engineering, Southwest Jiaotong University, Chengdu 610041 China.; Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Institute of Antibiotics, Chengdu University, Chengdu 610052 China
Abstract:An efficient and convenient method to construct tetracyclic isoquinolinium salts via [Cp*RhCl2]2 catalyzed C–H activation and [4 + 2] annulation reactions in ethanol is described. This reaction is very fast and highly efficient in the green solvent ethanol. The reaction works with a broad substrate scope affording the products in good to excellent yields in a short time. Moreover, a ratio of S/C up to 10 000 could be achieved with gram scale synthesis.

An efficient method to construct tetracyclic isoquinolinium salts via C–H activation and [4 + 2] annulation reactions in ethanol is described.
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