Cesium carbonate → 7-bromo-2-(3,5-difluoro-4-hydroxybenzyl)-2H-isoquinolin-3-one

HRID 488785ノート

反応式

HRID 488785 の反応式
[Br:1][C:2]1[CH:11]=[C:10]2[C:5]([CH:6]=[C:7]([OH:12])[N:8]=[CH:9]2)=[CH:4][CH:3]=1.Br[CH2:14][C:15]1[CH:20]=[C:19]([F:21])[C:18]([OH:22])=[C:17]([F:23])[CH:16]=1.C(=O)([O-])[O-].[Cs+].[Cs+]>CN(C)C=O>[Br:1][C:2]1[CH:3]=[CH:4][C:5]2[C:10]([CH:11]=1)=[CH:9][N:8]([CH2:14][C:15]1[CH:20]=[C:19]([F:21])[C:18]([OH:22])=[C:17]([F:23])[CH:16]=1)[C:7](=[O:12])[CH:6]=2

参加物

5

反応物 3

HCID 10796Cesium carbonateHCID 222653224-(Bromomethyl)-2,6-difluorophenolHCID 178515312HCID 178515312、化合物

生成物 1

HCID 222682637-bromo-2-(3,5-difluoro-4-hydroxybenzyl)-2H-isoquinolin-3-one

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

The alkylation of 7-bromo-3-hydroxy-isoquinoline (1.30 g, 5.80 mmol) using 4-bromomethyl-2,6-difluorophenol (1.68 g, 7.54 mmol) and cesium carbonate (2.46 g, 7.54 mmol) in dimethyl-formamide is carried out as previously described in Example 1, Step (1). The solid is collected by filtration, washed with water, ethyl acetate, and allowed to air dry under house vacuum. Drying will afford the desired product. Step (2): 2-(3,5-difluoro-4-hydroxybenzyl)-7-[3-(4H-[1,2,3]triazol-4-yl)prop-1-ynyl]-2H-isoquinolin-3-one

後処理

  1. filtrationThe solid is collected by filtration
  2. washwashed with water, ethyl acetate
  3. customto air dry under house vacuum
  4. customDrying will

出典と根拠

ORDレコード
ord-8eb7645f4e804a87a5da56d567a28410
出典データセット
uspto-grants-2005_12
特許番号
US06974822B2

反応ノート

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