Heating-induced decarboxylative cyclization for the synthesis of 5-trifluoromethyl-1,2,4-triazoles from trifluoroacetimidohydrazides and α-oxocarboxylic acids

Construction of trifluoromethyl-containing heterocycles from trifluoroacetimidoyl chlorides and derivatives

“…A heating-induced decarboxylative cyclization of trifluoroacetimidohydrazides and α-oxocarboxylic acids for the formation of 5-trifluoromethyl-1,2,4-triazoles under metal and additive-free conditions was disclosed by Wu, Chen and co-workers (Scheme 41). 53 The green protocol had the merits of readily available reactants, a broad substrate scope and operational simplicity. The ambient oxidative conditions or high temperature facilitated the C–C bond cleavage, thereby enabling the decarboxylation process.…”

Copper-Catalyzed Synthesis of 4-CF3-1,2,3-Triazoles: An Efficient and Facile Approach via Click Reaction

“…Since the time of its discovery in strategies to optimize the pharmacological properties of drug candidates [ 1 , 2 , 3 , 4 ], incorporation of the trifluoromethyl group has become a promising approach to discover new and/or improve existing bioactive compounds [ 5 , 6 , 7 , 8 ]. Although several valuable methods have been developed for the synthesis of trifluoromethyl-substituted compounds [ 9 , 10 , 11 , 12 , 13 , 14 , 15 , 16 , 17 , 18 , 19 , 20 ], methods that incorporate this group in an efficient and regiospecific manner remain in high demand [ 21 , 22 , 23 , 24 , 25 , 26 , 27 ], especially in the case of heterocyclic compounds [ 28 , 29 , 30 , 31 , 32 , 33 , 34 , 35 ].…”