Trifluoroacetic acid → 2-(2-(2-(piperidin-3-yl)-1H-benzo[d]imidazol-1-yl)ethyl)isoindoline-1,3-dione
反応式
[O:1]=[C:2]1[C:10]2[C:5](=[CH:6][CH:7]=[CH:8][CH:9]=2)[C:4](=[O:11])[N:3]1[CH2:12][CH2:13][N:14]1[C:18]2[CH:19]=[CH:20][CH:21]=[CH:22][C:17]=2[N:16]=[C:15]1[CH:23]1[CH2:28][CH2:27][CH2:26][N:25](C(OC(C)(C)C)=O)[CH2:24]1.FC(F)(F)C(O)=O>C(Cl)Cl>[NH:25]1[CH2:26][CH2:27][CH2:28][CH:23]([C:15]2[N:14]([CH2:13][CH2:12][N:3]3[C:4](=[O:11])[C:5]4[C:10](=[CH:9][CH:8]=[CH:7][CH:6]=4)[C:2]3=[O:1])[C:18]3[CH:19]=[CH:20][CH:21]=[CH:22][C:17]=3[N:16]=2)[CH2:24]1参加物
4
実験手順
tert-Butyl 3-(1-(2-(1,3-dioxoisoindolin-2-yl)ethyl)-1H-benzo[d]imidazol-2-yl)piperidine-1-carboxylate (129A) (4.36 mmoles max, crude mixture) was added to a 20 mL scintillation vial equipped for stirring. CH2Cl2 (3 mL) and trifluoroacetic acid (1 mL) were then added and the resultant solution was allowed to stir at room temperature for 72 hrs. The reaction was concentrated and dried in-vacuo affording 2-(2-(2-(piperidin-3-yl)-1H-benzo[d]imidazol-1-yl)ethyl)isoindoline-1,3-dione (129B) as a mixture that was used without further purification. ESI-MS: m/z 375.3 (M+H)+.