Ethanamine, 2,2,2-trifluoro- → HCID 46928967, compound

Participants

Reaction Conditions

Reaction Steps

Trimethylaluminium solution (2M in toluene, 0.8 mL, 1.60 mmol) was added to a solution of 2,2,2,-trifluoroethylamine (108 mg, 1.06 mmol) in dioxane (5 mL). The mixture was stirred for 1 h 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 (5 mL) was added. 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=2:3 to 3:2) to afford the title compound (70 mg, 59%) as a white solid. MS: m/e=444.2 [M+H]+.

Provenance & Evidence