反应详情

A stirred solution of 1-(2′,4-difluoro-1,1′-biphenyl-2-yl)ethylamine (0.26 g, 1.12 mmol) in dichloromethane (10 mL) was treated with 4-methoxybenzenesulfonyl chloride (0.23 g, 1.12 mmol), and pyridine (0.09 g, 1.12 mmol). The reaction was stirred at room temperature for twelve hours, diluted with dichloromethane, washed sequentially with a 1 N hydrochloric acid solution (2×) and a saturated, aqueous, sodium chloride solution. The organic phase was dried over anhydrous sodium sulfate, filtered through a short column of silica gel, and evaporated to a residue which, after crystallization from ethyl acetate-hexane, afforded the title compound (0.22 g, 0.53 mmol, 48%) as a racemic, homogeneous, colorless, crystalline solid, m.p. 182-184° C.;

1. washwashed sequentially with a 1 N hydrochloric acid solution (2×)
2. dry with materialThe organic phase was dried over anhydrous sodium sulfate
3. filtrationfiltered through a short column of silica gel
4. customevaporated to a residue which
5. customafter crystallization from ethyl acetate-hexane