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An efficient one-pot method for regio- and stereoselective synthesis of 5-(trifluoromethyl)-4,5,6,7-tetrahydro-[1,2,4]triazolo[1,5-a]pyrimidines under solvent-free and catalyst-free conditions has been developed. The method involves employing a three-component condensation reaction of an aromatic aldehyde and ethyl 4,4,4-trifluoro-3-oxobutanoate or 1,1,1-trifluoropentane-2,4-dione in the presence of 1,2,4-triazol-3-amine at 90°C.

chemical papers

A regio- and stereoselective three-component synthesis of 5-(trifluoromethyl)-4,5,6,7-tetrahydro-[1,2,4]triazolo[1,5-a]pyrimidine derivatives under solvent-free conditions