Triethylamine → (S)-1-Boc-3-methanesulfonyloxy-pyrrolidine
反応式
[OH:1][C@H:2]1[CH2:6][CH2:5][N:4]([C:7]([O:9][C:10]([CH3:13])([CH3:12])[CH3:11])=[O:8])[CH2:3]1.C(N(CC)CC)C.[CH3:21][S:22](Cl)(=[O:24])=[O:23]>C(Cl)Cl>[CH3:21][S:22]([O:1][C@H:2]1[CH2:6][CH2:5][N:4]([C:7]([O:9][C:10]([CH3:13])([CH3:12])[CH3:11])=[O:8])[CH2:3]1)(=[O:24])=[O:23]参加物
5
実験手順
To a stirred solution of (S)-tert-butyl 3-hydroxypyrrolidine-1-carboxylate (200 mg, 1.07 mmol) and triethylamine (0.3 mL, 1.07 mmol) in DCM (10 mL) at 0° C. was added methane sulfonylchloride (0.125 mL, 1.07 mmol) dropwise. After stirring for 3 h, the reaction mixture was washed with sat. NaHCO3 solution (aq.). The aqueous layer was extracted with DCM and the combined organics were dried (MgSO4), filtered and concentrated in vacuo to give the title compound (350 mg) as a colourless solid which was used in the next step without further purification.