1-(Thiazol-2-yl)piperazine → 5-chloro-3-(2-methoxyphenyl)-3-{2-oxo-2-[4-(1,3-thiazol-2-yl)piperazin-1-yl]ethyl}-1,3-dihydro-2H-indol-2-one

HRID 1662630ノート

反応式

HRID 1662630 の反応式
[Cl:1][C:2]1[CH:3]=[C:4]2[C:8](=[CH:9][CH:10]=1)[NH:7][C:6](=[O:11])[C:5]2([CH2:20][C:21](O)=[O:22])[C:12]1[CH:17]=[CH:16][CH:15]=[CH:14][C:13]=1[O:18][CH3:19].[S:24]1[CH:28]=[CH:27][N:26]=[C:25]1[N:29]1[CH2:34][CH2:33][NH:32][CH2:31][CH2:30]1>>[Cl:1][C:2]1[CH:3]=[C:4]2[C:8](=[CH:9][CH:10]=1)[NH:7][C:6](=[O:11])[C:5]2([C:12]1[CH:17]=[CH:16][CH:15]=[CH:14][C:13]=1[O:18][CH3:19])[CH2:20][C:21](=[O:22])[N:32]1[CH2:33][CH2:34][N:29]([C:25]2[S:24][CH:28]=[CH:27][N:26]=2)[CH2:30][CH2:31]1

参加物

3

反応物 2

HCID 9118061-(Thiazol-2-yl)piperazineHCID 21925457HCID 21925457、化合物

生成物 1

HCID 674300515-chloro-3-(2-methoxyphenyl)-3-{2-oxo-2-[4-(1,3-thiazol-2-yl)piperazin-1-yl]ethyl}-1,3-dihydro-2H-indol-2-one収率 83.8%

実験手順

With 800 mg of [5-chloro-3-(2-methoxyphenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]acetic acid, which is the compound described in Preparation 1.1 of the brochure Publication No. WO03/008407, and 449 mg of 1-(1,3-thiazol-2-yl)piperazine as starting materials, reaction manipulation and post-treatment were carried out by a similar method to Step 45-1, and the obtained residue was crystallized from EtOAc and n-hexane to obtain 976 mg of the title compound (colorless crystal).

後処理

  1. customdescribed in Preparation 1.1 of the brochure Publication No
  2. custommaterials, reaction manipulation
  3. customthe obtained residue was crystallized from EtOAc and n-hexane

出典と根拠

ORDレコード
ord-46a8850b980d423ea6cb203c3db53c68
出典データセット
uspto-grants-2011_10
特許番号
US08030499B2

反応ノート

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