2-(Aminomethyl)-5-methylpyrazine → 2-(4-Hydroxy-2-oxopyridin-1(2H)-yl)-4-methyl-N-((5-methylpyrazin-2-yl)methyl)thiazole-5-carboxamide

HRID 1887278

反応式

HRID 1887278 の反応式
[OH:1][C:2]1[CH:7]=[CH:6][N:5]([C:8]2[S:9][C:10]([C:14]([OH:16])=O)=[C:11]([CH3:13])[N:12]=2)[C:4](=[O:17])[CH:3]=1.[CH3:18][C:19]1[N:20]=[CH:21][C:22]([CH2:25][NH2:26])=[N:23][CH:24]=1>>[OH:1][C:2]1[CH:7]=[CH:6][N:5]([C:8]2[S:9][C:10]([C:14]([NH:26][CH2:25][C:22]3[CH:21]=[N:20][C:19]([CH3:18])=[CH:24][N:23]=3)=[O:16])=[C:11]([CH3:13])[N:12]=2)[C:4](=[O:17])[CH:3]=1

参加物

3

反応物 2

HCID 27564962-(Aminomethyl)-5-methylpyrazineHCID 547423412-(4-hydroxy-2-oxopyridin-1(2H)-yl)-4-methylthiazole-5-carboxylic acid

生成物 1

HCID 577444572-(4-Hydroxy-2-oxopyridin-1(2H)-yl)-4-methyl-N-((5-methylpyrazin-2-yl)methyl)thiazole-5-carboxamide収率 14%

実験手順

Following the procedure as described in Example 1, making variations only as required to use 2-(4-hydroxy-2-oxopyridin-1(2H)-yl)-4-methylthiazole-5-carboxylic acid in place of 4-methyl-2-(2-oxo-4-phenylpyridin-1(2H)-yl)thiazole-5-carboxylic acid to react with (5-methylpyrazin-2-yl)methanamine, the title compound was obtained as a colorless solid in 14% yield: 1H NMR (300 MHz, DMSO-d6) δ 11.49 (s, 1H), 8.80 (t, J=5.2 Hz, 1H), 8.59 (d, J=7.8 Hz 1H), 8.44 (s, 2H), 6.26 (d, J=7.8 Hz, 1H), 5.81 (s, 1H), 4.47 (d, J=5.2 Hz, 2H), 2.52 (s, 3H), 2.43 (s, 3H); MS (ES+) m/z 358.1 (M+1).

出典と根拠

ORDレコード
ord-ff040c22d3954d4ab2d916cbc46b8340
出典データセット
uspto-grants-2013_08
特許番号
US08501746B2

関連ノート

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