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

HRID 488785노트

반응식

HRID 488785 반응식
[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

참가 물질

5

반응물 3

HCID 10796Cesium carbonateHCID 222653224-(Bromomethyl)-2,6-difluorophenolHCID 178515312HCID 178515312, 화합물

생성물 1

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

시약·촉매·용매 1

HCID 6228Dimethylformamide용매

실험 절차

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

후처리

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

출처 및 근거

ORD 기록
ord-8eb7645f4e804a87a5da56d567a28410
출처 데이터셋
uspto-grants-2005_12
특허 번호
US06974822B2

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