5-chloro-2-(piperazine-1-sulfonyl)-1H-indole → 1-(5-Chloroindol-2-ylsulphonyl)-4-[4-(1-imidazolyl)benzoyl]piperazine

HRID 353460

反応式

HRID 353460 の反応式
Cl.[N:2]1([C:7]2[CH:15]=[CH:14][C:10]([C:11]([OH:13])=O)=[CH:9][CH:8]=2)[CH:6]=[CH:5][N:4]=[CH:3]1.[Cl:16][C:17]1[CH:18]=[C:19]2[C:23](=[CH:24][CH:25]=1)[NH:22][C:21]([S:26]([N:29]1[CH2:34][CH2:33][NH:32][CH2:31][CH2:30]1)(=[O:28])=[O:27])=[CH:20]2>CC(C)=O>[Cl:16][C:17]1[CH:18]=[C:19]2[C:23](=[CH:24][CH:25]=1)[NH:22][C:21]([S:26]([N:29]1[CH2:34][CH2:33][N:32]([C:11](=[O:13])[C:10]3[CH:9]=[CH:8][C:7]([N:2]4[CH:6]=[CH:5][N:4]=[CH:3]4)=[CH:15][CH:14]=3)[CH2:31][CH2:30]1)(=[O:28])=[O:27])=[CH:20]2

参加物

4

反応物 2

HCID 227105715-chloro-2-(piperazine-1-sulfonyl)-1H-indoleHCID 43810723HCID 43810723、化合物

生成物 1

HCID 99343981-(5-Chloroindol-2-ylsulphonyl)-4-[4-(1-imidazolyl)benzoyl]piperazine収率 60%

試薬・触媒・溶媒 1

HCID 180Acetone溶媒

実験手順

By an analogous method, starting from 4-(1-imidazolyl)benzoic acid hydrochloride and 1-(5-chloroindol-2-ylsulphonyl)piperazine, was prepared 1-(5-chloroindol-2-ylsulphonyl)-4-[4-(1-imidazolyl)benzoyl]piperazine (375 mg, 60% yield) as colourless crystals from acetone; m.p. 155-165° C., 1H NMR (d6DMSO) 3.0-3.2 ppm (broad s, 4H), 3.4-3.8 ppm (broad s, 4H), 7.0 ppm (s, 1H), 7.1 ppm (s, 1H), 7.3 ppm (dd, 1H), 7.5 ppm (m, 3H), 7.7 ppm (d, 2H), 7.8 ppm (m, 2M), 8.3 ppm (s, 1H), 12.4 ppm (broad s, 1H), the spectrum also contained a signal due to acetone, ca 0.05 mol. eq.; MS (M+H)+ 470/472.

出典と根拠

ORDレコード
ord-82bc999cf39849ac8078170352e6c961
出典データセット
uspto-grants-2004_06
特許番号
US06753331B1

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