Sodium Hydroxide → (2R)-2-[(4-{[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino}quinazolin-5-yl)oxy]propanoic acid
反応式
[N:1]1[CH:6]=[CH:5][CH:4]=[CH:3][C:2]=1[CH2:7][N:8]1[C:16]2[C:11](=[CH:12][C:13]([NH:17][C:18]3[C:27]4[C:22](=[CH:23][CH:24]=[CH:25][C:26]=4[O:28][C@H:29]([CH3:34])[C:30]([O:32]C)=[O:31])[N:21]=[CH:20][N:19]=3)=[CH:14][CH:15]=2)[CH:10]=[N:9]1.[OH-].[Na+]>CO>[N:1]1[CH:6]=[CH:5][CH:4]=[CH:3][C:2]=1[CH2:7][N:8]1[C:16]2[C:11](=[CH:12][C:13]([NH:17][C:18]3[C:27]4[C:22](=[CH:23][CH:24]=[CH:25][C:26]=4[O:28][C@H:29]([CH3:34])[C:30]([OH:32])=[O:31])[N:21]=[CH:20][N:19]=3)=[CH:14][CH:15]=2)[CH:10]=[N:9]1参加物
4
実験手順
To a stirred solution of methyl (2R)-2-[(4-{[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino}quinazolin-5-yl)oxy]propanoate (520 mg, 1.15 mmol) (obtained as described in example 1, preparation of starting materials) in methanol (10 ml), was added 2.5M aqueous sodium hydroxide (2 ml, 5 mmol) and the solution was stirred for 3 hours. The solution was evaporated and the residue was taken into water and was acidified to about pH4 with acetic acid and stirred for 15 minutes. The precipitate was filtered off, washed with water and dried to provide (2R)-2-[(4-{[1-(pyridin-2-ylmethyl)-1H-indazol-5-yl]amino}quinazolin-5-yl)oxy]propanoic acid, (435 mg, 86%); NMR spectrum (300 MHz) 1.69 (d, 3H), 5.36 (q, 1H), 5.75 (s, 2H), 6.94 (d, 1H), 7.14 (d, 1H), 7.27 (t, 1H), 7.35 (d, 1H), 7.71 (m, 4H), 8.12 (s, 1H), 8.43 (s, 1H), 8.52 (s, 2H), 10 76 (s, 1H), one exchangeable not observed; Mass spectrum MH+ 441.