HCID 66813055、化合物 → HCID 44515079、化合物

反応式

[F:1][C:2]1[CH:3]=[C:4]([CH:8]([O:25][C:26]2[CH:27]=[C:28]3[C:32](=[CH:33][CH:34]=2)[N:31]([C:35]2[CH:40]=[CH:39][C:38]([F:41])=[CH:37][CH:36]=2)[N:30]=[CH:29]3)[C@@H:9]([NH:19][C:20](=[O:24])[CH2:21][O:22][CH3:23])[CH2:10][O:11]CC2C=CC=CC=2)[CH:5]=[CH:6][CH:7]=1.[H][H]>C(O)C.[Pd]>[F:1][C:2]1[CH:3]=[C:4]([CH:8]([O:25][C:26]2[CH:27]=[C:28]3[C:32](=[CH:33][CH:34]=2)[N:31]([C:35]2[CH:36]=[CH:37][C:38]([F:41])=[CH:39][CH:40]=2)[N:30]=[CH:29]3)[C@@H:9]([NH:19][C:20](=[O:24])[CH2:21][O:22][CH3:23])[CH2:10][OH:11])[CH:5]=[CH:6][CH:7]=1

参加物

実験手順

N-[(1S)-2-(3-Fluorophenyl)-2-{[1-(4-fluorophenyl)-1H-indazole-5-yl]oxy}-1-(benzyloxymethyl)ethyl]-2-methoxyacetamide (15 mg, 0.027 mmol) is dissolved in 10 mL ethanol and Pd (10% on charcoal, 0.29 mg, 0.0027 mmol) is added. The reaction mixture is charged with hydrogen and stirred for 2 h at r.t. After filtration of the reaction mixture via a glass microfibre filter, the solvent evaporated and the residue purified by chromatography (silicagel, eluents: ethylacetate/hexane). 7.5 mg (59.6%) of the title compound as a mixture of stereoisomers are obtained.