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[F:1][C:2]([F:12])([F:11])[C:3]1[CH:10]=[CH:9][C:6]([CH2:7]Br)=[CH:5][CH:4]=1.[CH2:13]([NH:20][C:21]([C:23]1[S:27][C:26]([N:28]2[CH:33]=[CH:32][C:31]([OH:34])=[CH:30][C:29]2=[O:35])=[N:25][C:24]=1[CH3:36])=[O:22])[C:14]1[CH:19]=[CH:18][CH:17]=[CH:16][CH:15]=1>>[CH2:13]([NH:20][C:21]([C:23]1[S:27][C:26]([N:28]2[CH:33]=[CH:32][C:31]([O:34][CH2:7][C:6]3[CH:9]=[CH:10][C:3]([C:2]([F:12])([F:11])[F:1])=[CH:4][CH:5]=3)=[CH:30][C:29]2=[O:35])=[N:25][C:24]=1[CH3:36])=[O:22])[C:14]1[CH:19]=[CH:18][CH:17]=[CH:16][CH:15]=1참가 물질
실험 절차
Following the procedure as described in Example 9, making variations only as required to use 4-trifluoromethylbenzyl bromide in place of 2-cyclopropylethyl 4-methylbenzenesulfonate to react with N-benzyl-2-(4-hydroxy-2-oxopyridin-1(2H)-yl)-4-methylthiazole-5-carboxamide, the title compound was obtained as a colorless solid in 21% yield: mp 278-280° C.; 1H NMR (300 MHz, DMSO-d6) δ 8.78 (br s, 1H), 8.65-8.62 (m, 1H), 7.78-7.64 (m, 4H), 7.30-7.29 (m, 5H), 6.44-6.41 (m, 1H), 6.23 (d, J=2.7 Hz, 1H), 5.30 (s, 2H), 4.38 (d, J=6.0 Hz, 2H), 2.54 (s, 3H); 13C NMR (75 MHz, DMSO-d6) δ 167.3, 161.9, 161.6, 153.9, 150.4, 140.7, 139.9, 132.3, 128.8, 128.7, 127.7, 127.2, 126.4, 126.0, 125.9, 123.8, 104.3, 97.7, 69.8, 43.1, 17.5; MS (ES+) m/z 500.3 (M+1).
출처 및 근거
- ORD 기록
- ord-5bfa2ba951794d4c8b1e38ae46d9a61b
- 출처 데이터셋
- uspto-grants-2013_08
- 특허 번호
- US08501746B2
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