Synthesis of difluoromethylated benzylborons via rhodium(Ⅰ)-catalyzed fluorine-retainable hydroboration of gem-difluoroalkenes  

作　　者：Yuanhong Cai Donghang Tan Qiqi Zhang Wenxin Lv Qingjiang Li Honggen Wang 

机构地区：[1]Guangdong Provincial Key Laboratory of Chiral Molecule and Drug Discovery,School of Pharmaceutical Sciences,Sun Yat-sen University.Guangzhou 510006,China [2]State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources,School of Chemistry and Pharmaceutical Sciences of Guangxi Normal University,Guilin 541004,China

出　　处：《Chinese Chemical Letters》2021年第1期417-420,共4页中国化学快报（英文版）

基　　金：financial support from the National Natural Science Foundation of China(No.21971261);Guangdong Provincial Key Laboratory of Chiral Molecule and Drug Discovery(No.2019B030301005);Key Project of Chinese National Programs for Fundamental Research and Development(No.2016YFA0602900);the Local Innovative and Research Teams Project of Guangdong Pearl River Talents Program(No.2017BT01Y093)is gratefully acknowledged。

摘　　要：The synthesis of bo rylated orga nofluorines is of great interest due to their potential values as synthons in modular construction of fluorine-containing molecules.Reported herein is a rhodium-catalyzed hydrobo ration of arylgem-difluoroalkenes leading to a series of α-difluoromethylated benzylborons.The use of cationic rhodium catalyst and a biphosphine ligand with large bite angle was crucial for reactivity by offering good regioselectivity and diminishing the undesired β-F elimination.Preliminary derivatizations of the products were conducted to showcase the utility of this protocol.

关 键 词：RHODIUM HYDROBORATION Difluoromethy gem-Difluoroalkene β-F elimination 

分 类 号：TQ460.1[化学工程—制药化工]