反应 #1435753

反应方程式

3-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-propylamine dihydrochloride

N,N-diisopropylethylamine

3-Chloro-4,6-difluorobenzenesulfonyl chloride

→

solid

收率 87.0%

5-Chloro-N-[3-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-propyl]-2,4-difluoro-benzenesulfonamide

收率 87.0%

溶剂

CH2Cl2

反应条件

后处理

1. 1
   洗涤The resulting solution was washed with water (3×20 mL)
2. 2
   干燥dried over Na2SO4
3. 3
   其他evaporated to dryness
4. 4
   workup.DISSOLUTIONThe free base was dissolved in 2-propanol (5 mL)
5. 5
   其他The product was crystallized in 2-propanol (5 mL)
6. 6
   过滤collected by filtration, and vacuum
7. 7
   其他dried

实验过程

A solution of 3-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-propylamine dihydrochloride (323 mg, 1 mmol), N,N-diisopropylethylamine (517 mg, 4 mmol) in CH2Cl2(15 mL), was added 3-Chloro-4,6-difluorobenzenesulfonyl chloride (259 mg, 1.05 mmol) and was stirred overnight at room temperature. The resulting solution was washed with water (3×20 mL) and dried over Na2SO4, and evaporated to dryness. The free base was dissolved in 2-propanol (5 mL). The product was crystallized in 2-propanol (5 mL) collected by filtration, and vacuum dried to give a white solid (401 mg, 87%).

来源