UMR 6014 CNRS COBRA, Normandie Université, INSA Rouen , 1 rue Tesnière, 76821 Mont Saint Aignan, France.
Department of Nanopharmaceutical Sciences, Nagoya Institute of Technology , Gokiso, Showa-ku, Nagoya 466-8555, Japan.
Org Lett. 2016 May 20;18(10):2467-70. doi: 10.1021/acs.orglett.6b01026. Epub 2016 Apr 28.
The regioselective trifluoromethylthiolation of indole derivatives was achieved under reductive conditions with trifluoromethanesulfonyl chloride as the readily available source of electrophilic SCF3 and a phosphine as the reducing agent. It is a straightforward process free from any metal and also applicable for the trifluoromethylthiolation of other azaarenes, enamines, and enoxysilanes.
在还原条件下，使用三氟甲磺酸氯作为易得的亲电 SCF3 源，以及膦作为还原剂，实现了吲哚衍生物的区域选择性三氟甲硫基化。这是一个简单的过程，无需任何金属，也适用于其他氮杂芳烃、烯胺和烯氧基硅烷的三氟甲硫基化。
