Trifluoromethyl-Substituted Pyridines Through Displacement of Iodine by in situ Generated (Trifluoromethyl)copper

Recent advances in the trifluoromethylation methodology and new CF3-containing drugs

“…The key fluorine-containing block 2,4-dichloro-5-(trifluoromethyl)pyrimidine (37) used in this procedure is commercially available. It can be prepared by chlorination of 5-TFU (5-trifluoromethyluracil) (38) with phosphorus oxychloride in 95% yield [107] (Scheme 17, path a).…”

Decarboxylative trifluoromethylation of aryl halides using well-defined copper–trifluoroacetate and –chlorodifluoroacetate precursors

“…The catalytic trifluoromethylation of non-activated organic halides represents a long-standing goal in organometallic chemistry [1][2][3][4][5][6][7][8][9][10]. The ability to introduce a trifluoromethyl group into a molecule of interest at a late stage of a synthesis using mild conditions alleviates the need to carry the fluorine functional group through potentially incompatible synthetic procedures, thereby eliminating potential side-reactions and raising overall yields.…”

The solid complex Zn(CF3)Br·2DMF as an alternative reagent for the preparation of both, trifluoromethyl and pentafluoroethyl copper, CuCF3 and CuC2F5

“…Some publications [7][8][9][10][11] show that the formation of CuCF 3 can be achieved using the commercially available compound Me 3 SiCF 3 either starting from copper alkoxides [8,9] or the system of heavier copper halides and an alkali fluoride [7,10,11].…”