D-Lactic Acid → (2R)-N-[(1R,2S)-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-(3-methoxyphenyl)propan-2-yl]-2-hydroxy-propanamide
反応式
[OH:1][C@H:2]([CH3:6])[C:3](O)=[O:4].[F:7][C:8]1[CH:13]=[CH:12][C:11]([N:14]2[C:22]3[C:17](=[CH:18][C:19]([O:23][C@H:24]([C:28]4[CH:33]=[CH:32][CH:31]=[C:30]([O:34][CH3:35])[CH:29]=4)[C@@H:25]([NH2:27])[CH3:26])=[CH:20][CH:21]=3)[CH:16]=[N:15]2)=[CH:10][CH:9]=1>C1COCC1>[F:7][C:8]1[CH:9]=[CH:10][C:11]([N:14]2[C:22]3[C:17](=[CH:18][C:19]([O:23][C@H:24]([C:28]4[CH:33]=[CH:32][CH:31]=[C:30]([O:34][CH3:35])[CH:29]=4)[C@@H:25]([NH:27][C:3](=[O:4])[C@H:2]([OH:1])[CH3:6])[CH3:26])=[CH:20][CH:21]=3)[CH:16]=[N:15]2)=[CH:12][CH:13]=1参加物
4
実験手順
To a stirred solution of 1,1-carbonyldiimidazole (31 mg, 190 μmol) in THF (1 ml) was added (2R)-2-hydroxypropanoic acid (18 mg, 20 μmol) to give a colorless solution. The reaction mixture was stirred for 1 h at r.t. Then a solution of (1R,2S)-1-{[1-(4-fluorophenyl)-1H-indazol-5-yl]oxy}-1-(3-methoxyphenyl)propan-2-amine (6a, 39 mg, 100 μmol) in THF (0.5 ml) was added, and the stirring was continued at r.t. overnight. The solvent was removed in vacuo, the residue dissolved in acetonitrile/water mixture, and the crude product purified by preparative HPLC. Yield 16 mg (35%).