3-(Methyl(phenyl)amino)-3-oxopropanoic acid → N1-(4-(2-(2,2-Dimethylhydrazinecarbonyl)thieno[3,2-b]pyridin-7-yloxy)-3-fluorophenyl)-N3-methyl-N3-phenylmalonamide

HRID 2193738ノート

反応式

HRID 2193738 の反応式
[CH3:1][N:2]([CH3:38])[NH:3][C:4]([C:6]1[S:14][C:13]2[C:8](=[N:9][CH:10]=[CH:11][C:12]=2[O:15][C:16]2[CH:21]=[CH:20][C:19]([NH:22][C:23](=[O:36])[CH2:24][C:25]([NH:27][C:28]3[CH:33]=[CH:32][CH:31]=[CH:30][C:29]=3OC)=[O:26])=[CH:18][C:17]=2[F:37])[CH:7]=1)=[O:5].[CH3:39]N(C1C=CC=CC=1)C(=O)CC(O)=O>>[CH3:1][N:2]([CH3:38])[NH:3][C:4]([C:6]1[S:14][C:13]2[C:8](=[N:9][CH:10]=[CH:11][C:12]=2[O:15][C:16]2[CH:21]=[CH:20][C:19]([NH:22][C:23](=[O:36])[CH2:24][C:25]([N:27]([CH3:39])[C:28]3[CH:29]=[CH:30][CH:31]=[CH:32][CH:33]=3)=[O:26])=[CH:18][C:17]=2[F:37])[CH:7]=1)=[O:5]

参加物

3

反応物 2

HCID 3500563-(Methyl(phenyl)amino)-3-oxopropanoic acidHCID 16040873N1-(4-(2-(2,2-Dimethylhydrazinecarbonyl)thieno[3,2-b]pyridin-7-yloxy)-3-fluorophenyl)-N3-(2-methoxyphenyl)malonamide

生成物 1

HCID 16040874N1-(4-(2-(2,2-Dimethylhydrazinecarbonyl)thieno[3,2-b]pyridin-7-yloxy)-3-fluorophenyl)-N3-methyl-N3-phenylmalonamide収率 44%

実験手順

Following the procedure described above for compound 236 (example 95, scheme 63) but replacing acid 27 with 3-(methyl(phenyl)amino)-3-oxopropanoic acid (31), title compound 240 was obtained in 44% yield. 1H NMR (400 MHz, DMSO-d6) δ (ppm): 10.36 (s, 1H), 10.08 (br, 0.3H), 9.52 (s, 0.7H), 8.58 (dd, J=5.5 Hz, 3=8.4 Hz, 1H), 8.20 (m, 1H), 7.79 (m, 1H), 7.49-7.30 (m, 7H), 6.75 (d, J=5.5 Hz, 1H), 3.21 (s, 2H), 3.2 (s, 3H), 2.64 (s, 3H) 2.59 (s, 3H). MS (m/z): (M+1) 522.1 (100%).

出典と根拠

ORDレコード
ord-e5c0e877319143c4829ead8a86a9f649
出典データセット
uspto-grants-2012_12
特許番号
US08329726B2

反応ノート

読み込み中…