3-Methylthiophene-2-sulfonamide → HCID 69144749、化合物

HRID 1593058

反応式

HRID 1593058 の反応式
[S:1](=[N:4][C:5]([NH2:7])=[O:6])(=[O:3])=[O:2].C(OC(=O)[N:14]([C:16]1[CH:17]=[C:18]2[C:23](=[CH:24][C:25]=1[F:26])[C:22](=[O:27])[N:21]([C:28]1[CH:33]=[CH:32][C:31](N)=[CH:30][CH:29]=1)[CH:20]=[CH:19]2)C)(C)(C)C.[CH3:36][C:37]1[CH:41]=[CH:40][S:39][C:38]=1S(N)(=O)=O>>[NH2:14][C:16]1[CH:17]=[C:18]2[C:23](=[CH:24][C:25]=1[F:26])[C:22](=[O:27])[N:21]([C:28]1[CH:33]=[CH:32][C:31]([NH:7][C:5]([NH:4][S:1]([C:38]3[S:39][CH:40]=[CH:41][C:37]=3[CH3:36])(=[O:3])=[O:2])=[O:6])=[CH:30][CH:29]=1)[CH:20]=[CH:19]2

参加物

4

反応物 3

HCID 3410833-Methylthiophene-2-sulfonamideHCID 118190831-SulfonylureaHCID 58998471[2-(4-Amino-phenyl)-7-fluoro-1-oxo-1,2-dihydro-isoquinolin-6-yl]-methyl-carbamic acid tert-butyl ester

生成物 1

HCID 69144749HCID 69144749、化合物

実験手順

An analogous sulfonylurea coupling and de-protection procedure to that described in Example 29 was performed on [2-(4-Amino-phenyl)-7-fluoro-1-oxo-1,2-dihydro-isoquinolin-6-yl]-methyl-carbamic acid tert-butyl ester (Example 9) and 3-methyl-thiophene-2-sulfonamide to give N-({[4-(6-amino-7-fluoro-1-oxoisoquinolin-2(1H)-yl)phenyl]amino}carbonyl)-3-methylthiophene-2-sulfonamide. ES-MS (M+H)+=487.1; 1H-NMR (DMSO-d6) δ (ppm): 8.96-8.92 (bs, 1H), 7.86-7.82 (d, J=5.1 Hz, 1H), 7.66-7.60 (d, J=12.4 Hz, 1H), 7.46-7.40 (m, 2H), 7.32-7.26 (m, 2H), 7.24-7.20 (d, J=7.3 Hz, 1H), 7.03-7.00 (d, J=5.1 Hz, 1H), 6.72-6.68 (d, J=8.8 Hz, 1H), 6.56-6.48 (bs, 1H), 6.50-6.46 (d, J=7.7 Hz, 1H), 2.82-2.78 (bd, J=4.8 Hz, 3H), 2.45-2.43 (s, 3H).

出典と根拠

ORDレコード
ord-c081237a08bb4a0ea129f2e91746b16d
出典データセット
uspto-grants-2007_11
特許番号
US07294635B2

関連ノート

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