1616729-59-9Relevant academic research and scientific papers
Nickel-catalyzed cross-coupling of functionalized difluoromethyl bromides and chlorides with aryl boronic acids: A general method for difluoroalkylated arenes
Xiao, Yu-Lan,Guo, Wen-Hao,He, Guo-Zhen,Pan, Qiang,Zhang, Xingang
supporting information, p. 9909 - 9913,5 (2014/12/09)
Transition-metal-catalyzed difluoroalkylation of aromatics remains challenging despite the importance of difluoroalkylated arenes in medicinal chemistry. Herein, the first successful example of nickel-catalyzed difluoroalkylation of aryl boronic acids is described. The reaction allows access to a variety of functionalized difluoromethyl bromides and chlorides, and paves the way to highly cost-efficient synthesis of a wide range of difluoroalkylated arenes. The notable features of this protocol are its high generality, excellent functional-group compatibility, low-cost nickel-catalyst, and practicality for gram-scale production, thus providing a facile method for applications in drug discovery and development.
Heteroaryldifluoromethylation of organoborons catalyzed by palladium: Facile access to aryl(heteroaryl)difluoromethanes
Xiao, Yu-Lan,Zhang, Bo,Feng, Zhang,Zhang, Xingang
supporting information, p. 4822 - 4825 (2015/04/27)
A first example of Pd-catalyzed heteroaryldifluoromethylation of organoborons with bromodifluoromethylated heteroarenes has been described. The use of phosphine ligand PAd2(n-Bu)·HI is critical for the reaction efficiency. With use of this ligand, a wide range of aryl(heteroaryl)-difluoromethanes were obtained with high efficiency. The notable features of this reaction are its broad substrate scope and excellent functional group compatibility, thus providing a facile protocol for application in drug discovery and development.
Highly effective copper-mediated gem-difluoromethylenation of arylboronic acids
Ma, Guobin,Wan, Wen,Hu, Qingyang,Jiang, Haizhen,Wang, Jing,Zhu, Shizheng,Hao, Jian
supporting information, p. 7527 - 7530 (2014/07/07)
A copper-mediated gem-difluoromethylenation of aryl, heteroaryl and vinyl boronic acids with bromodifluoromethylated oxazole or thiazole derivatives has been developed. This novel reaction showed an excellent functional group tolerance and wide substrate scope, providing facile access to practical application in drug discovery and development. the Partner Organisations 2014.
