Isoxazole, 4-(chloromethyl)-3,5-dimethyl- → N-benzyl-2-(4-((3,5-dimethylisoxazol-4-yl)methoxy)-2-oxopyridin-1(2H)-yl)-4-methylthiazole-5-carboxamide

HRID 1887348

反応式

HRID 1887348 の反応式
Cl[CH2:2][C:3]1[C:4]([CH3:9])=[N:5][O:6][C:7]=1[CH3:8].[CH2:10]([NH:17][C:18]([C:20]1[S:24][C:23]([N:25]2[CH:30]=[CH:29][C:28]([OH:31])=[CH:27][C:26]2=[O:32])=[N:22][C:21]=1[CH3:33])=[O:19])[C:11]1[CH:16]=[CH:15][CH:14]=[CH:13][CH:12]=1>>[CH2:10]([NH:17][C:18]([C:20]1[S:24][C:23]([N:25]2[CH:30]=[CH:29][C:28]([O:31][CH2:2][C:3]3[C:4]([CH3:9])=[N:5][O:6][C:7]=3[CH3:8])=[CH:27][C:26]2=[O:32])=[N:22][C:21]=1[CH3:33])=[O:19])[C:11]1[CH:16]=[CH:15][CH:14]=[CH:13][CH:12]=1

参加物

3

反応物 2

HCID 88246Isoxazole, 4-(chloromethyl)-3,5-dimethyl-HCID 54742338N-benzyl-2-(4-hydroxy-2-oxopyridin-1(2H)-yl)-4-methylthiazole-5-carboxamide

生成物 1

HCID 57744482N-benzyl-2-(4-((3,5-dimethylisoxazol-4-yl)methoxy)-2-oxopyridin-1(2H)-yl)-4-methylthiazole-5-carboxamide収率 10%

実験手順

Following the procedure as described in Example 21, making variation only as required to use 4-(chloromethyl)-3,5-dimethylisoxazole in place of 2-(chloromethyl)-5-phenyl-1,3,4-oxadiazole 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 10% yield: 1H NMR (300 MHz, CDCl3) δ 8.69 (d, J=8.1 Hz, 1H), 7.41-7.26 (m, 5H), 6.16-6.06 (m, 3H), 4.76 (s, 2H), 4.59 (d, J=5.5 Hz, 2H), 2.68 (s, 3H), 2.41 (s, 3H), 2.27 (s, 3H); MS (ES+) m/z 451.1 (M+1).

出典と根拠

ORDレコード
ord-f4521b2c34724f008cf7aaa171fa8603
出典データセット
uspto-grants-2013_08
特許番号
US08501746B2

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