[O:1]=[C:2]1[N:6]2[C:7]3[CH:14]=[CH:13][C:12]([N:15]4[CH2:20][CH2:19][O:18][CH2:17][C:16]4=[O:21])=[CH:11][C:8]=3[O:9][CH2:10][C@H:5]2[C@H:4]([CH2:22][N:23]2C(=O)C3C(=CC=CC=3)C2=O)[O:3]1.C(Cl)Cl.CO>C(O)C>[NH2:23][CH2:22][C@H:4]1[C@H:5]2[N:6]([C:7]3[CH:14]=[CH:13][C:12]([N:15]4[CH2:20][CH2:19][O:18][CH2:17][C:16]4=[O:21])=[CH:11][C:8]=3[O:9][CH2:10]2)[C:2](=[O:1])[O:3]1Compound 2-(((3S,3aS)-1-oxo-7-(3-oxomorpholin-4-yl)-1,3,3a,4-tetrahydrobenzo[b]oxazolo[3,4-d][1,4]oxazin-3-yl)methyl)isoindolin-1,3-dione (3.71 g, 8.263 mmol) prepared as above in (d) was partly dissolved in 50 ml of ethanol. 60 ml of methylamine alcohol solution was added and the mixture was allowed to react under reflux at 78° C. for 3 h. TLC (DCM/MeOH=10/1) was employed to monitor the reaction. After the reaction completed, the solvent was evaporated, and the remainder was directly subjected to the next step of reaction.
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