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 69514ノート

反応式

HRID 69514 の反応式
[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

参加物

5

反応物 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

生成物 1

HCID 579169512-{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

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

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+).

後処理

  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

出典と根拠

ORDレコード
ord-517bee44a03549aa958ccded15dc44c2
出典データセット
uspto-grants-2014_09
特許番号
US08822495B2

反応ノート

読み込み中…