反应详情

To a solution of 2-(1-benzyl-3-hydroxypyrrolidin-3-yl)-N-(tert-butyl)benzene sulfonamide (350 mg, 0.00090 mol) in acetonitrile (15 mL, 0.29 mol) were added sodium iodide (418 mg, 0.00279 mol) and chlorotrimethylsilane (0.354 mL, 0.00279 mol). The reaction mixture was refluxed under nitrogen for 1 hour and then cooled down to room temperature, then quenched with 10% aqueous sodium thiosulfate solution (10 mL), and then extracted with EtOAc. The organic phase was washed with water then brine, and then dried over MgSO4 followed by filteration. The filtrate was concentrated to give the desired compound (170 mg, 60% yield). MS (ESI): 315.0 (M+H+).

1. temperatureThe reaction mixture was refluxed under nitrogen for 1 hour
2. customquenched with 10% aqueous sodium thiosulfate solution (10 mL)
3. extractionextracted with EtOAc
4. washThe organic phase was washed with water
5. dry with materialbrine, and then dried over MgSO4
6. concentrationThe filtrate was concentrated