HCID 15524163, 화합물 → Methyl 2-[({4-[1-(t-butoxycarbonyl)propyl]benzenesulfonylamino}carbonyl)amino]-4-chlorobenzoate
반응식
[NH2:1][S:2]([C:5]1[CH:10]=[CH:9][C:8]([CH:11]([CH2:19][CH3:20])[C:12]([O:14][C:15]([CH3:18])([CH3:17])[CH3:16])=[O:13])=[CH:7][CH:6]=1)(=[O:4])=[O:3].[Cl:21][C:22]1[CH:23]=[C:24]([NH:32][C:33](OC2C=CC=CC=2)=[O:34])[C:25](=[CH:30][CH:31]=1)[C:26]([O:28][CH3:29])=[O:27]>>[C:15]([O:14][C:12]([CH:11]([C:8]1[CH:7]=[CH:6][C:5]([S:2]([NH:1][C:33]([NH:32][C:24]2[CH:23]=[C:22]([Cl:21])[CH:31]=[CH:30][C:25]=2[C:26]([O:28][CH3:29])=[O:27])=[O:34])(=[O:3])=[O:4])=[CH:10][CH:9]=1)[CH2:19][CH3:20])=[O:13])([CH3:16])([CH3:18])[CH3:17]참가 물질
3
실험 절차
From 1.02 g (3.41 mmol) of tert-butyl (±)-2-(4-aminosulfonylphenyl)butyrate and 1.04 g (3.41 mmol) of methyl 4-chloro-2-N-phenoxycarbonylanthranilate in a manner similar to Preparation Example 1, 1.46 g (yield 84%) of methyl 2-[({4-[1-(t-butoxycarbonyl)propyl]benzenesulfonylamino}carbonyl)amino]-4-chlorobenzoate (property: colorless amorphous, PMR (δppm, CDCl3): 0.89 (3H, t), 1.38 (9H, s), 1.69-1.76 (1H, m), 2.03-2.10 (1H, m), 3.42 (1H, t), 3.94 (3H, s), 7.04 (1H, d), 7.47 (2H, d), 7.93 (1H, d), 8.01 (2H, d), 8.45 (1H, br), 11.04 (1H, br)) was obtained. Then, 4.3 ml (8.6 mmol) of 2N sodium hydroxide was used in a similar manner to prepare 1.43 g of a carboxylic acid. Using 463 mg (2.86 mmol) of CDI, 970 mg (yield 71%: 2 steps) of (±)-2-{4-[(7-chloro-2,4(1H,3H)-quinazoline-3-yl)sulfonyl]phenyl}butyric acid t-butylester was obtained.