Methanol → 6-((1S,3S)-3-Amino-cyclopentyloxy)-2H-isoquinolin-1-one
反応式
COC1C=CC(C[N:8]2[CH:17]=[CH:16][C:15]3[C:10](=[CH:11][CH:12]=[C:13]([O:18][C@H:19]4[CH2:23][CH2:22][C@H:21]([NH2:24])[CH2:20]4)[CH:14]=3)[C:9]2=[O:25])=CC=1.CO>C(O)(C(F)(F)F)=O>[NH2:24][C@H:21]1[CH2:22][CH2:23][C@H:19]([O:18][C:13]2[CH:14]=[C:15]3[C:10](=[CH:11][CH:12]=2)[C:9](=[O:25])[NH:8][CH:17]=[CH:16]3)[CH2:20]1参加物
4
反応条件
- 温度
- 150 °C
実験手順
125 mg (0.34 mmol) of 2-(4-methoxy-benzyl)-6-((1S,3S)-3-amino-cyclopentyloxy)-2H-isoquinolin-1-one (39) were dissolved in 1 mL of TFA and heated in a microwave oven at 150° C. for 3 h. Methanol was added and the reaction mixture was evaporated. The solution was taken up in 1N HCl and extracted three times with dichloromethane. The combined dichloromethane layers were extracted with 1N HCl twice and the combined HCl layers were lyophilized. The residue was dissolved in water and lyophilized again to yield 42 mg of 6-((1S,3S)-3-amino-cyclopentyloxy)-2H-isoquinolin-1-one (43) as hydrochloride. Rt=0.86 min (Method E). Detected mass: 245.1 (M+H+).