Cesium carbonate → 4-(2-Methoxy-4-{1-oxo-6-[(S)-1-(tetrahydro-furan-2-yl)methoxy]-1H-isoquinolin-2-yl}-phenyl)-[1,4]diazepane-1-carboxylic acid 3-fluoro-propyl ester

HRID 69517Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 69517
[N:1]1([C:8]2[CH:13]=[CH:12][C:11]([N:14]3[CH:23]=[CH:22][C:21]4[C:16](=[CH:17][CH:18]=[C:19]([O:24][CH2:25][C@@H:26]5[CH2:30][CH2:29][CH2:28][O:27]5)[CH:20]=4)[C:15]3=[O:31])=[CH:10][C:9]=2[O:32][CH3:33])[CH2:7][CH2:6][CH2:5][NH:4][CH2:3][CH2:2]1.Br[CH2:35][CH2:36][CH2:37][F:38].[C:39](=O)([O-:41])[O-:40].[Cs+].[Cs+]>CN(C=O)C>[F:38][CH2:37][CH2:36][CH2:35][O:41][C:39]([N:4]1[CH2:5][CH2:6][CH2:7][N:1]([C:8]2[CH:13]=[CH:12][C:11]([N:14]3[CH:23]=[CH:22][C:21]4[C:16](=[CH:17][CH:18]=[C:19]([O:24][CH2:25][C@@H:26]5[CH2:30][CH2:29][CH2:28][O:27]5)[CH:20]=4)[C:15]3=[O:31])=[CH:10][C:9]=2[O:32][CH3:33])[CH2:2][CH2:3]1)=[O:40]

Komponenten

5

Edukt 3

HCID 10796Cesium carbonateHCID 67699Propane, 1-bromo-3-fluoro-HCID 689913772-(4-[1,4]Diazepan-1-yl-3-methoxy-phenyl)-6-[(S)-1-(tetrahydro-furan-2-yl)methoxy]-2H-isoquinolin-1-one

Produkt 1

HCID 579167194-(2-Methoxy-4-{1-oxo-6-[(S)-1-(tetrahydro-furan-2-yl)methoxy]-1H-isoquinolin-2-yl}-phenyl)-[1,4]diazepane-1-carboxylic acid 3-fluoro-propyl ester

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 6228DimethylformamideLösungsmittel

Versuchsvorschrift

To a solution of 2-(4-[1,4]Diazepan-1-yl-3-methoxy-phenyl)-6-[(S)-1-(tetrahydro-furan-2-yl)methoxy]-2H-isoquinolin-1-one (50 mg) and 1-Bromo-3-fluoro-propane (18 mg) in DMF (1 mL) was added cesium carbonate (54 mg) and the mixture was stirred overnight. The crude mixture was purified by preparative HPLC. The product with the molecular weight of 553.64 (C30H36FN3O6) was obtained in this way; MS (ESI): 554 (M+H+).

Aufarbeitung

  1. customThe crude mixture was purified by preparative HPLC
  2. customThe product with the molecular weight of 553.64 (C30H36FN3O6) was obtained in this way

Quellen und Nachweise

ORD-Eintrag
ord-5f99bf5486a64320862b253200e73e5d
Quelldatensatz
uspto-grants-2014_09
Patentnummer
US08822495B2

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