N-(2-Methoxy-phenyl)-malonamic acid → N1-(3-Fluoro-4-(2-(1-isopropyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yloxy)phenyl)-N3-(2-methoxyphenyl)malonamide

HRID 418641노트

반응식

HRID 418641 반응식
[F:1][C:2]1[CH:3]=[C:4]([CH:6]=[CH:7][C:8]=1[O:9][C:10]1[CH:15]=[CH:14][N:13]=[C:12]2[CH:16]=[C:17]([C:19]3[N:20]=[CH:21][N:22]([CH:24]([CH3:26])[CH3:25])[CH:23]=3)[S:18][C:11]=12)[NH2:5].FC1C=CC=CC=1NC(=O)CC(O)=O.[CH3:41][O:42][C:43]1[CH:48]=[CH:47][CH:46]=[CH:45][C:44]=1[NH:49][C:50](=[O:55])[CH2:51][C:52](O)=[O:53]>>[F:1][C:2]1[CH:3]=[C:4]([NH:5][C:52](=[O:53])[CH2:51][C:50]([NH:49][C:44]2[CH:45]=[CH:46][CH:47]=[CH:48][C:43]=2[O:42][CH3:41])=[O:55])[CH:6]=[CH:7][C:8]=1[O:9][C:10]1[CH:15]=[CH:14][N:13]=[C:12]2[CH:16]=[C:17]([C:19]3[N:20]=[CH:21][N:22]([CH:24]([CH3:26])[CH3:25])[CH:23]=3)[S:18][C:11]=12

참가 물질

4

반응물 3

HCID 12664594N-(2-Methoxy-phenyl)-malonamic acidHCID 164811562-[(2-Fluorophenyl)carbamoyl]acetic acidHCID 587903973-Fluoro-4-(2-(1-isopropyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yloxy)aniline

생성물 1

HCID 16041964N1-(3-Fluoro-4-(2-(1-isopropyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yloxy)phenyl)-N3-(2-methoxyphenyl)malonamide

실험 절차

Title compound 126 (scheme 36) was obtained similarly to the compound 122 (example 45, scheme 36) starting from the amine 125 and replacing the acid 29 with the acid 27. 1H NMR (DMSO-d6). δ (ppm): 10.58 (s, 1H), 9.64 (s, 1H), 8.43 (d, J=5.6 Hz, 1H), 8.07 (dd, J=1.6 and 7.2 Hz, 1H), 8.05 (d, J=1.2 Hz, 1H), 7.87 (dd, J=2.4 and 12.8 Hz, 1H), 7.84 (d, J=1.2 Hz, 1H), 7.67 (s, 1H), 7.49 (t, J=8.8 Hz, 1H), 7.43 (dd, J=1.6 and 8.8 Hz, 1H), 7.12-7.04 (m, 2H), 6.92 (ddd, J=2.4, 7.2 and 8.8 Hz, 1H), 6.58 (d, J=5.6 Hz, 1H), 4.48 (quin, J=6.4 Hz, 1H), 3.86 (s, 3H), 3.64 (s, 2H), 1.46 (d, J=6.8 Hz, 6H). MS (m/z): 559.2 (M+H).

출처 및 근거

ORD 기록
ord-761b3419302049ac9644d8c115bf9c39
출처 데이터셋
uspto-grants-2012_01
특허 번호
US08093264B2

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