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 1662630노트

반응식

HRID 1662630 반응식
[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

참가 물질

3

반응물 2

HCID 9118061-(Thiazol-2-yl)piperazineHCID 21925457HCID 21925457, 화합물

생성물 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-one수율 83.8%

실험 절차

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).

후처리

  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

출처 및 근거

ORD 기록
ord-46a8850b980d423ea6cb203c3db53c68
출처 데이터셋
uspto-grants-2011_10
특허 번호
US08030499B2

반응 노트

불러오는 중…