反应 #1885096

反应方程式

1-(5-Iodo-2-methyl-phenyl)-4-(toluene-4-sulfonyl)-piperazine

sodium 3-(difluoromethoxy)benzenesulfinate

cesium carbonate

→

product

收率 63.1%

1-[5-(3-Difluoromethoxy-benzenesulfonyl)-2-methyl-phenyl]-4-(toluene-4-sulfonyl)-piperazine

收率 63.1%

溶剂

toluene

反应条件

后处理

1. 1
   过滤The reaction mixture was filtered
2. 2
   其他the solvent evaporated
3. 3
   其他The crude product was purified via silica gel chromatography with toluene/methanol 20:1 (2.5% triethylamine), fractions
4. 4
   workup.ADDITIONcontaining the product
5. 5
   其他the solvents evaporated

实验过程

0.521 g of 1-(5-Iodo-2-methyl-phenyl)-4-(toluene-4-sulfonyl)-piperazine (1.14 mmol), 0.315 g of sodium 3-(difluoromethoxy)benzenesulfinate (1.37 mmol), 0.558 g of cesium carbonate (1.713 mmol), 0.026 g of Pd(dba)3 (0.029 mmol), 0.033 g of Xantphos (0.059 mmol) and 0.381 g of tetrabutylammonium chloride (1.37 mmol) were stirred for 8 h in 10 mL of toluene. The reaction mixture was filtered and the solvent evaporated. The crude product was purified via silica gel chromatography with toluene/methanol 20:1 (2.5% triethylamine), fractions containing the product combined and the solvents evaporated to yield 0.386 g of product.

来源