Diisopropylethylamine → 6-[3-(4-Fluoro-phenyl)-5-methyl-3H-[1,2,3]-triazol-4-ylmethoxy]-N-(tetrahydro-pyran-4-yl)-nicotinamide

Participants

Reaction Steps

To a solution of 6-[3-(4-fluoro-phenyl)-5-methyl-3H-[1,2,3]triazol-4-ylmethoxy]-nicotinic acid (83 mg, 0.25 mmol) and TBTU (90 mg, 0.28 mmol) in DMF (3.0 mL) was added DIPEA (217 μL, 1.26 mmol). Then 4-aminotetrahydropyran (28 mg, 0.28 mmol) was added and the mixture was stirred at room temperature under Ar for 30 min. The mixture was then evaporated and purification by chromatography (silica, 50 to 100% ethyl acetate in heptane) afforded the title compound (100 mg, 96%) as a white solid. MS: m/e=412.3 [M+H]+.

Provenance & Evidence