反应详情

To a stirred solution of (RS)-2-(3-fluoro-phenyl)-pyrrolidine (0.24 g, 1.45 mmol) and triethylamine (0.40 ml, 2.87 mmol) in dichloromethane (40 ml) was added at 0° C. toluene-4-sulfonyl chloride (0.42 g, 2.20 mmol). The mixture was stirred at RT for 16 h, evaporated, dissolved in water (40 ml) and extracted with ethyl acetate (2×40 ml). The combined organic layers were washed with water (40 ml), brine (40 ml), dried (MgSO4) and evaporated. The crude product was purified by crystallization from ethyl acetate/hexane to give the product (0.38 g, 83%) as a white solid, m.p. 116° C. and MS: m/e=319 (M+).

1. customevaporated
2. dissolutiondissolved in water (40 ml)
3. extractionextracted with ethyl acetate (2×40 ml)
4. washThe combined organic layers were washed with water (40 ml), brine (40 ml)
5. dry with materialdried (MgSO4)
6. customevaporated
7. customThe crude product was purified by crystallization from ethyl acetate/hexane