Cu-Mediated Chemoselective Trifluoromethylation of Benzyl Bromides Using Shelf-Stable Electrophilic Trifluoromethylating Reagents

被引:109
作者
Kawai, Hiroyuki [1 ]
Furukawa, Tatsuya [1 ]
Nomura, Yoshinori [1 ]
Tokunaga, Etsuko [1 ]
Shibata, Norio [1 ]
机构
[1] Nagoya Inst Technol, Grad Sch Engn, Dept Frontier Mat, Showa Ku, Nagoya, Aichi 4668555, Japan
关键词
CATALYZED TRIFLUOROMETHYLATION; ENANTIOSELECTIVE TRIFLUOROMETHYLATION; ORGANIC HALIDES; NUCLEOPHILIC TRIFLUOROMETHYLATION; CONFIGURATIONAL STABILITY; REDUCTIVE ELIMINATION; MEDICINAL CHEMISTRY; CONVENIENT METHOD; BORONIC ACIDS; SALT SYSTEM;
D O I
10.1021/ol201205t
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Copper-mediated chemoselective trifluoromethylation at the benzylic :position by the use of shelf-stable electrophilic trifluoromethylating reagents 3 in good to high yields under mild conditions is described for the first time. The generality of this trifluoromethylation for a wide variety of benzyl bromides facilitates the rapid creation of structural diversity of medicinal candidates in drug discovery.
引用
收藏
页码:3596 / 3599
页数:4
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