N1-(3-Fluoro-4-(2-(1-methyl-1H-imidazol-2-yl)thieno[3,2-b]pyridin-7-yloxy)phenyl)-N3-(2-methoxyphenyl)malonamide → N1-(3-Fluoro-4-(2-(1-methyl-1H-imidazol-5-yl)thieno[3,2-b]pyridin-7-yloxy)phenyl)-N3-(2-methoxyphenyl)malonamide

反応式

[F:1][C:2]1[CH:3]=[C:4]([NH:24][C:25](=[O:38])[CH2:26][C:27]([NH:29][C:30]2[CH:35]=[CH:34][CH:33]=[CH:32][C:31]=2[O:36][CH3:37])=[O:28])[CH:5]=[CH:6][C:7]=1[O:8][C:9]1[CH:14]=[CH:13][N:12]=[C:11]2[CH:15]=[C:16](C3N(C)C=CN=3)[S:17][C:10]=12.FC1C=C(N)C=CC=1OC1C=CN=C2C=C([C:56]3[N:60]([CH3:61])[CH:59]=[N:58][CH:57]=3)SC=12>>[F:1][C:2]1[CH:3]=[C:4]([NH:24][C:25](=[O:38])[CH2:26][C:27]([NH:29][C:30]2[CH:35]=[CH:34][CH:33]=[CH:32][C:31]=2[O:36][CH3:37])=[O:28])[CH:5]=[CH:6][C:7]=1[O:8][C:9]1[CH:14]=[CH:13][N:12]=[C:11]2[CH:15]=[C:16]([C:56]3[N:60]([CH3:61])[CH:59]=[N:58][CH:57]=3)[S:17][C:10]=12

参加物

反応物 2

HCID 16040869N1-(3-Fluoro-4-(2-(1-methyl-1H-imidazol-2-yl)thieno[3,2-b]pyridin-7-yloxy)phenyl)-N3-(2-methoxyphenyl)malonamide

HCID 594244313-Fluoro-4-(2-(1-methyl-1H-imidazol-5-yl)thieno[3,2-b]pyridin-7-yloxy)benzenamine

生成物 1

HCID 16040871N1-(3-Fluoro-4-(2-(1-methyl-1H-imidazol-5-yl)thieno[3,2-b]pyridin-7-yloxy)phenyl)-N3-(2-methoxyphenyl)malonamide収率 24%

実験手順

Following the procedure described above for the compound 28a (example 8, step 2) but replacing amine 9 for amine 18, title compound 28c was obtained in 24% yield. 1H NMR (DMSO-d6) δ (ppm): 10.58 (s, 1H), 9.62 (s, 1H), 8.49 (d, 1H), 8.05 (dd, 1H), 7.85 (m, 2H), 7.77 (s, 1H), 7.48 (t, 1H), 7.41 (m, 2H), 7.05 (m, 2H), 6.90 (m, 2H) 6.63 (dd, 1H), 3.88 (s, 3H), 3.84 (s, 3H), 3.63 (s, 2H). MS (m/z): 531.8 (M+H).

出典と根拠

ORDレコード: ord-3c13b45f3946450a93bef49a97e20c28
出典データセット: uspto-grants-2012_01
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US08093264B2

反応ノート

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