1-Sulfonylurea → HCID 69434770、化合物

HRID 1593057ノート

反応式

HRID 1593057 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.[Cl: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:29]=[CH:30][C:31]([NH:7][C:5]([NH:4][S:1]([C:38]3[S:39][CH:40]=[CH:41][C:37]=3[Cl:36])(=[O:3])=[O:2])=[O:6])=[CH:32][CH:33]=1)[CH:20]=[CH:19]2

参加物

4

反応物 3

HCID 118190831-SulfonylureaHCID 233580193-Chlorothiophene-2-sulfonamideHCID 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 69434770HCID 69434770、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) using 3-chloro-thiophene-2-sulfonic acid amide as the coupling partner to give N-({[4-(6-amino-7-fluoro-1-oxoisoquinolin-2(1H)-yl)phenyl]amino}carbonyl)-3-chlorothiophene-2-sulfonamide. ES-MS (M+H)+=507.0, 509.0 (Cl); 1H-NMR (DMSO-d6) δ (ppm): 8.98-8.91 (bs, 1H), 8.06-7.98 (m, 1H), 7.66-7.60 (d, J=12.8 Hz, 1H), 7.48-7.40 (d, J=8.8 Hz, 2H), 7.30-7.25 (d, J=8.8 Hz, 2H), 7.24-7.20 (m, 1H), 7.24-7.18 (d, J=7.3 Hz, 1H), 6.72-6.66 (d, J=8.4 Hz, 1H), 6.56-6.48 (bs, 1H), 6.50-6.46 (d, J=7.3 Hz, 1H), 2.82-2.75 (s, 3H).

出典と根拠

ORDレコード
ord-dde067fd00ae4255ac6e4c33a8038d15
出典データセット
uspto-grants-2007_11
特許番号
US07294635B2

反応ノート

読み込み中…