State Key Laboratory of Structural Chemistry, Center for Excellence in Molecular Synthesis, Fujian Institute of Research on the Structure of Matter, Chinese Academy of Sciences, Fuzhou 350002, China.
University of Chinese Academy of Sciences, Beijing 100049, China.
Org Lett. 2021 Jun 4;23(11):4191-4196. doi: 10.1021/acs.orglett.1c01103. Epub 2021 May 12.
A Rh-catalyzed decarbonylative C-H coupling of -generated acid fluorides with amide substrates bearing -Csp-H bonds has been developed. This method enables alkyl, aryl, and alkenyl carboxylic acids to undergo decarbonylative coupling with C-H bonds of (hetero)aromatic or alkenyl amides in generally good yields via the conversion of carboxylic acids into acid fluorides and also allows for the functionalization of a series of structurally complex carboxyl-containing natural products and pharmaceuticals as well as pharmaceutical amide derivatives.
发展了一种 Rh 催化的生成的酸氟化物与酰胺底物中 -Csp-H 键的脱羰基 C-H 键偶联反应。该方法通过将羧酸转化为酸氟化物,使烷基、芳基和烯基羧酸与(杂)芳基或烯基酰胺的 C-H 键进行脱羰基偶联,一般产率良好,同时也允许一系列结构复杂的含羧基天然产物和药物以及药物酰胺衍生物的功能化。