反应详情

To 2-(4-((5-(2-(4-chloro-3-methoxyphenyl)propan-2-yl)-1-(4-fluorophenyl)-1H-imidazol-2-ylthio)methyl)-3,5-difluorophenoxy)ethanol (270 mg, 0.48 mmol, 1.0 eq) in DCM (2.5 mL) was added methanesulfonyl chloride (0.1 mL, 1.44 mmol, 3.0 eq), followed by diisopropylamine (0.25 mL, 1.44 mmol, 3.0 eq). The reaction mixture was stirred at room temperature for 45 min at which time LCMS showed complete consumption of starting material. Aqueous work up (EtOAc and water) followed by purification (column chromatography, 0 to 80% EtOAc/Hex) provided 2-(4-((5-(2-(4-chloro-3-methoxyphenyl)propan-2-yl)-1-(4-fluorophenyl)-1H-imidazol-2-ylthio)methyl)-3,5-difluorophenoxy)ethyl methanesulfonate (230 mg, 75%) as a white foam. MS (EI) m/z 462 (MH+).

1. customconsumption of starting material
2. customAqueous work up (EtOAc and water) followed by purification (column chromatography, 0 to 80% EtOAc/Hex)