2,2,3,3,3-Pentafluoropropylamine → HCID 46929059, compound

Participants

Reaction Conditions

Reaction Steps

Trimethylaluminium solution (2M in toluene, 0.80 mL, 1.60 mmol) was added to a solution of 2,2,3,3,3-pentafluoropropylamine (116 μL, 1.10 mmol) in dioxane (4 mL). The mixture was stirred for 45 min at 50° C. Then a solution of 6-[3-(3,4-difluoro-phenyl)-5-hydroxymethyl-isoxazol-4-ylmethoxy]-nicotinic acid methyl ester (100 mg, 0.27 mmol) in dioxane (4 mL) was added and the reaction mixture was stirred overnight at 85° C. The dioxane was removed by distillation. The remaining material was purified by chromatography (silica, ethyl acetate:heptane=1:1) to afford the title compound (96 mg, 73%) as a white solid. MS: m/e=492.1 [M−H]−.

Provenance & Evidence