Potassium Carbonate → 4-(2-{1-[1-(4-Chloro-phenyl)-cyclobutyl]-3,4-dihydro-isoquinolin-7-yloxy}-acetyl)-piperazine-1-carboxylic acid tert-butyl ester

HRID 242052

반응식

HRID 242052 반응식
[Cl:1][C:2]1[CH:7]=[CH:6][C:5]([C:8]2([C:12]3[C:21]4[C:16](=[CH:17][CH:18]=[C:19]([OH:22])[CH:20]=4)[CH2:15][CH2:14][N:13]=3)[CH2:11][CH2:10][CH2:9]2)=[CH:4][CH:3]=1.[C:23]([O:27][C:28]([N:30]1[CH2:35][CH2:34][N:33]([C:36](=[O:39])[CH2:37]Cl)[CH2:32][CH2:31]1)=[O:29])([CH3:26])([CH3:25])[CH3:24].C(=O)([O-])[O-].[K+].[K+]>CN(C)C=O>[C:23]([O:27][C:28]([N:30]1[CH2:31][CH2:32][N:33]([C:36](=[O:39])[CH2:37][O:22][C:19]2[CH:20]=[C:21]3[C:16]([CH2:15][CH2:14][N:13]=[C:12]3[C:8]3([C:5]4[CH:4]=[CH:3][C:2]([Cl:1])=[CH:7][CH:6]=4)[CH2:11][CH2:10][CH2:9]3)=[CH:17][CH:18]=2)[CH2:34][CH2:35]1)=[O:29])([CH3:26])([CH3:24])[CH3:25]

참가 물질

5

반응물 3

HCID 11430Potassium CarbonateHCID 15829156tert-Butyl 4-(chloroacetyl)piperazine-1-carboxylateHCID 582462431-[1-(4-Chlorophenyl)cyclobutyl]-3,4-dihydroisoquinolin-7-ol

생성물 1

HCID 582463044-(2-{1-[1-(4-Chloro-phenyl)-cyclobutyl]-3,4-dihydro-isoquinolin-7-yloxy}-acetyl)-piperazine-1-carboxylic acid tert-butyl ester

시약·촉매·용매 1

HCID 6228Dimethylformamide용매

실험 절차

1-[1-(4-chlorophenyl)cyclobutyl]-3,4-dihydroisoquinolin-7-ol (example 82) (400 mg, 1.18 mmol) and 4-(2-chloro-acetyl)-piperazine-1-carboxylic acid tert-butyl ester (404 mg, 1.54 mmol) were dissolved in N,N-dimethyl-formamide (10 ml). After addition of potassium carbonate (355 mg, 2.57 mmol) the mixture was stirred for 2 h under reflux. The solvent was removed and the residue (690 mg) was used in the next step without further purification.

후처리

  1. temperatureunder reflux
  2. customThe solvent was removed
  3. customthe residue (690 mg) was used in the next step without further purification

출처 및 근거

ORD 기록
ord-593aec18e6744c4bbc03311d83fcc721
출처 데이터셋
uspto-grants-2014_02
특허 번호
US08653100B2

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