Ammonium Hydroxide → Tert-butyl 4-(5-(2-aminonicotinoyl)thiazol-2-yl)-1,4-diazepane-1-carboxylate
反応式
[C:1]([O:5][C:6]([N:8]1[CH2:14][CH2:13][CH2:12][N:11]([C:15]2[S:16][C:17]([C:20](=[O:28])[C:21]3[CH:26]=[CH:25][CH:24]=[N:23][C:22]=3F)=[CH:18][N:19]=2)[CH2:10][CH2:9]1)=[O:7])([CH3:4])([CH3:3])[CH3:2].[OH-].[NH4+:30]>>[C:1]([O:5][C:6]([N:8]1[CH2:14][CH2:13][CH2:12][N:11]([C:15]2[S:16][C:17]([C:20](=[O:28])[C:21]3[CH:26]=[CH:25][CH:24]=[N:23][C:22]=3[NH2:30])=[CH:18][N:19]=2)[CH2:10][CH2:9]1)=[O:7])([CH3:4])([CH3:3])[CH3:2]参加物
3
反応条件
- 温度
- 110 °C
実験手順
A microwave vial was charged with tert-butyl-4-(5-(2-fluoronicotinoyl)thiazol-2-yl)-1,4-diazepane-1-carboxylate (300 mg, 0.75 mmol) and aqueous ammonium hydroxide (1 ml). The reaction mixture was stirred in the microwave at 110° C. for 25 minutes. The reaction mixture was concentrated in vacuo to afford the title compound (300 mg, 100%). The residue was used in the next step without any further purification. MS (ES+): 405