Isopropylamine → 5-[5-(4-Fluoro-phenyl)-3-methyl-3H-[1,2,3]triazol-4-ylmethoxy]-pyrazine-2-carboxylic acid isopropylamide

Participants

Reaction Steps

To a solution of 5-[5-(4-fluoro-phenyl)-3-methyl-3H-[1,2,3]triazol-4-ylmethoxy]-pyrazine-2-carboxylic acid (96 mg, 0.29 mmol) and TBTU (103 mg, 0.32 mmol) in DMF (1.5 mL) was added DIPEA (250 μL, 1.46 mmol). Then isopropylamine (27 μL, 0.32 mmol) was added and the mixture was stirred at room temperature under Ar for 1 h. The mixture was then evaporated and purification by chromatography (silica, 50 to 100% ethyl acetate in heptane) afforded the title compound (53 mg, 49%) as a white solid after recrystallisation from ethyl acetate/heptane. MS: m/e=371.3 [M+H]+.

Provenance & Evidence