反应详情

A solution of tert-butyl 2-methyl-4-(2-oxo-1,3,4-oxathiazol-5-yl)benzoate (50 mg) in 1,3-dichloro-5-[1-(trifluoromethyl)vinyl]benzene (5 mL, prepared according to WO 2005085216) was heated 190° C. during 10 minutes in a microwave. The residue was purified by chromatography on silica gel (eluent: cyclohexane/ethyl acetate) then on preparative HPLC to give tert-butyl 4-[5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4H-isothiazol-3-yl]-2-methyl-benzoate (18.5 mg) as a solid. 1H-NMR (CDCl3, 400 MHz): δ=7.86 (d, 1 H), 7.54-7.64 (m, 2 H), 7.41 (t, 1 H), 7.31 (s, 2 H), 4.23 (d, 1 H), 3.88 (d, 1 H), 2.61 (s, 3 H), 1.61 ppm (s, 9 H).

1. customThe residue was purified by chromatography on silica gel (eluent: cyclohexane/ethyl acetate)