2-Methoxyethanol → 2-Methoxyethyl 3-{[(5-chloro-3-methyl-1-benzothiophen-2-yl)sulfonyl]amino}benzoate
反応式
[Cl:1][C:2]1[CH:3]=[CH:4][C:5]2[S:9][C:8]([S:10]([NH:13][C:14]3[CH:15]=[C:16]([CH:20]=[CH:21][CH:22]=3)[C:17]([OH:19])=[O:18])(=[O:12])=[O:11])=[C:7]([CH3:23])[C:6]=2[CH:24]=1.[CH3:25][O:26][CH2:27][CH2:28]O>>[Cl:1][C:2]1[CH:3]=[CH:4][C:5]2[S:9][C:8]([S:10]([NH:13][C:14]3[CH:15]=[C:16]([CH:20]=[CH:21][CH:22]=3)[C:17]([O:19][CH2:28][CH2:27][O:26][CH3:25])=[O:18])(=[O:12])=[O:11])=[C:7]([CH3:23])[C:6]=2[CH:24]=1参加物
3
実験手順
The product was prepared from 3-{[(5-chloro-3-methyl-1-benzothien-2-yl)sulfonyl]amino}benzoic acid (21 mg, 0.055 mmol) (Intermediate 19) and 2-methoxyethanol (7.6 mg, 0.100 mmol) according to the General Procedure 7, described in Example 107. The title compound was obtained in 70% yield (16.9 mg). 1H NMR (500 MHz, CDCl3) δ ppm 2.47 (s, 3 H) 3.40 (s, 3 H) 3.67-3.70 (m, 2 H) 4.42-4.45 (m, 2 H) 6.92 (s, 1 H) 7.37 (dd, J=8.02, 7.74 Hz, 1 H) 7.45 (dd, J=8.73, 1.96 Hz, 1 H) 7.45 (ddd, J=8.02, 2.34, 1.17 Hz, 1 H) 7.72 (dd, J=8.73, 0.60 Hz, 1 H) 7.72 (dd, J=1.96, 0.60 Hz, 1 H) 7.74 (dd, J=2.34, 1.59 Hz, 1 H) 7.87 (ddd, J=7.74, 1.59, 1.17 Hz, 1 H). MS (ESI+) m/z 440 [M+H]+.