Oxolan-3-amine → 3-[3-(5-Fluoro-pyridin-2-yl)-5-methyl-isoxazol-4-ylmethoxy]-isothiazole-5-carboxylic acid (tetrahydro-furan-3-yl)-amide

Participants

Reaction Steps

As described for example 38b, 3-[3-(5-fluoro-pyridin-2-yl)-5-methyl-isoxazol-4-ylmethoxy]-isothiazole-5-carboxylic acid methyl ester (120 mg, 0.34 mmol), was converted, using 3-aminotetrahydrofuran (36 mg, 0.41 mmol), instead of isopropyl amine, to the title compound (38 mg, 27%) which was obtained as a white solid after purification by chromatography (silica, heptane:ethyl acetate=75:25 to 25:75). MS: m/e=405.3 [M+H]+.

Provenance & Evidence