[NH2:1][CH:2]1[CH2:7][CH2:6][N:5]([C:8]2[N:13]=[C:12]([C:14]3[C:22]4[C:17](=[CH:18][CH:19]=[C:20]([C:23]([O:25]C)=[O:24])[CH:21]=4)[NH:16][CH:15]=3)[CH:11]=[N:10][CH:9]=2)[CH2:4][CH2:3]1.[OH-].[Na+].Cl>C1COCC1>[NH2:1][CH:2]1[CH2:3][CH2:4][N:5]([C:8]2[N:13]=[C:12]([C:14]3[C:22]4[C:17](=[CH:18][CH:19]=[C:20]([C:23]([OH:25])=[O:24])[CH:21]=4)[NH:16][CH:15]=3)[CH:11]=[N:10][CH:9]=2)[CH2:6][CH2:7]1To mixture of methyl 3-(6-(4-aminopiperidin-1-yl)pyrazin-2-yl)-1H-indole-5-carboxylate (236) (60 mg, 0.17 mmol) in THF (1 mL) was added 10% NaOH solution (1 mL). The reaction mixture was heated at 60° C. for 24 h and cooled to 0° C. 1N HCl solution was added to the mixture to attain pH7. The resulting mixture was stirred at RT for 2 h. The resulting precipitate was collected by filtration, washed with water and dried under vacuum to obtain the title compound (30 mg, 57%). MS (ESI, pos. ion) m/z: 337.9 (M+1).
読み込み中…
