2-Dimethylaminopyridine → (αR,βR)-β-(2,5-Difluorophenyl)-β-hydroxy-α-methyl-1H-1,2,4-triazole-1-butanamide

Participants

Reaction Steps

7.1 g (25.4 mmol) of (3R,4R)-4-(2,5-difluorophenyl)-3-methyl-4-[1,2,4]triazol-1-ylmethyl-oxetan-2-one were dissolved in 250 ml aqueous ammonia (NH4OH 25%) and, after the addition of 64 mg (0.5 mmol) of dimethylaminopyridine, were stirred for 1 hour at room temperature. Evaporation of the reaction mixture gave crude 7.55 g (100% yield) of (2R,3R)-3-(2,5-difluoro-phenyl)-3-hydroxy-2-methyl-4-[1,2,4]triazol-1-yl-butyramide.

Provenance & Evidence