CO[C:3](=[O:19])[CH2:4][CH:5]1[CH2:9][CH2:8][N:7]([CH2:10][CH2:11][C:12]2[CH:17]=[CH:16][CH:15]=[CH:14]C=2)[C:6]1=[O:18].CO.[NH2:22][O:23][K].C(O)(=O)C>CO.C(Cl)(Cl)Cl>[CH2:10]([N:7]1[CH2:8][CH2:9][CH:5]([CH2:4][C:3]([NH:22][OH:23])=[O:19])[C:6]1=[O:18])[C:11]1[CH:12]=[CH:17][CH:16]=[CH:15][CH:14]=112 mg of (2-oxo-1-phenethyl-pyrrolidin-3-yl)-acetic acid methyl ester (25r) prepared by the above Step 1 was dissolved in methanol solution (0.04 mmol) and then 1.7 M methanolic suspension solution containing NH2OK (0.07 ml, 0.12 mmol) was added thereto at 0° C. and the resulting mixture was stirred for 4 hrs at room temperature. The resulting mixture was neutralized with 0.02 ml of acetic acid, diluted with 10% methanol/chloroform solution, filtered and concentrated in vacuo. The resulting compound was purified by Silica gel column chromatography with a solvent mixture mixed with methanol and chloroform (1:9) as an eluant to give 1.6 mg of 2-(1-benzyl-2-oxo-pyrrolidin-3-yl)-N-hydroxy-acetamide (25s) (yield: 8%).
読み込み中…
