Trifluoroacetic acid → HCID 89963038, 화합물

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[CH3:1][O:2][C:3]1[CH:41]=[C:40]([O:42][CH3:43])[CH:39]=[CH:38][C:4]=1[CH2:5][N:6]([C:32]1[CH:37]=[CH:36][N:35]=[CH:34][N:33]=1)[S:7]([C:10]1[C:11]([F:31])=[CH:12][C:13]([O:19][C@H:20]2[CH2:24][CH2:23][CH2:22][C@@H:21]2[C:25]2[N:29]([CH3:30])[N:28]=[CH:27][CH:26]=2)=[C:14]([CH:18]=1)[C:15]([NH2:17])=O)(=[O:9])=[O:8].C(N(CC)CC)C.FC(F)(F)C(O)=O>ClCCl>[C:15]([C:14]1[C:13]([O:19][C@H:20]2[CH2:24][CH2:23][CH2:22][C@@H:21]2[C:25]2[N:29]([CH3:30])[N:28]=[CH:27][CH:26]=2)=[CH:12][C:11]([F:31])=[C:10]([S:7]([N:6]([CH2:5][C:4]2[CH:38]=[CH:39][C:40]([O:42][CH3:43])=[CH:41][C:3]=2[O:2][CH3:1])[C:32]2[CH:37]=[CH:36][N:35]=[CH:34][N:33]=2)(=[O:8])=[O:9])[CH:18]=1)#[N:17]

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실험 절차

To a solution of the 5-{[(2,4-dimethoxybenzyl)(pyrimidin-4-yl)amino]sulfonyl}-4-fluoro-2-{[(1S*,2R*)-2-(1-methyl-1H-pyrazol-5-yl)cyclopentyl]oxy}benzamide (64.3 mg, 0.107 mmol) prepared in Example 62c in dichloromethane (2.0 mL), triethylamine (41.0 μL, 0.300 mmol) and trifluoroacetic acid (21.0 μL, 0.150 mmol) were added with cooling on ice, and the reaction solution was stirred at room temperature for 2 hours. To the reaction solution, triethylamine (41.0 μL, 0.300 mmol) and trifluoroacetic acid (21.0 μL, 0.150 mmol) were added, and the mixture was stirred at room temperature for 1 hour. The reaction solution was purified with silica gel chromatography (ethyl acetate) to yield the title compound (32.3 mg, 53%) as a colorless oil.