反应详情

To a solution of 2,2,2-trifluoro-1-{4-[(6-fluoropyridin-2-yl)oxy]-3-methoxyphenyl}ethanol (0.52 mmol; 165 mg), tosyl chloride (0.57 mmol; 109 mg) and DMAP (0.01 mmol; 1.5 mg) under argon in dichloromethane (4 mL) at 0° C. was added TEA (1.04 mmol; 145 μl). The reaction mixture was stirred at rt for 3 h, then washed with brine (2×), dried over MgSO4, concentrated and purified by preparative TLC on silica gel (ethyl acetate/cyclohexane—30/70) to yield the title compound (101 mg; 0.21 mmol; 41%).

1. washwashed with brine (2×)
2. dry with materialdried over MgSO4
3. concentrationconcentrated
4. custompurified by preparative TLC on silica gel (ethyl acetate/cyclohexane—30/70)