Cesium carbonate → 2-{4-[4-(3-Fluoro-propyl)-[1,4]diazepan-1-yl]-3-methoxy-phenyl}-6-[(S)-1-(tetrahydro-furan-2-yl)methoxy]-2H-isoquinolin-1-one

HRID 69514Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 69514
[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(=O)([O-])[O-].[Cs+].[Cs+]>CN(C=O)C>[F:38][CH2:37][CH2:36][CH2:35][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

Komponenten

5

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 509.63 (C29H36FN3O4) was obtained in this way; MS (ESI): 510 (M+H+).

Aufarbeitung

  1. customThe crude mixture was purified by preparative HPLC
  2. customThe product with the molecular weight of 509.63 (C29H36FN3O4) was obtained in this way

Quellen und Nachweise

ORD-Eintrag
ord-517bee44a03549aa958ccded15dc44c2
Quelldatensatz
uspto-grants-2014_09
Patentnummer
US08822495B2

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