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 1850832Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 1850832
[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]

Komponenten

5

Edukt 3

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

Produkt 1

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

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 6228DimethylformamideLösungsmittel

Versuchsvorschrift

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.

Aufarbeitung

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

Quellen und Nachweise

ORD-Eintrag
ord-010002d815d644bb9fba98044da078fc
Quelldatensatz
uspto-grants-2015_02
Patentnummer
US08957089B2

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