反应 #554647

反应方程式

5-bromo-2-chloropyrimidine

cyclopropyl boronic acid

K3PO4

tricyclohexylphosphine

→

2-Chloro-5-cyclopropylpyrimidine

溶剂

toluene

water

反应条件

后处理

1. 1
   其他The mixture is degassed thoroughly
2. 2
   其他After degassing again the mixture
3. 3
   过滤filtered
4. 4
   其他the solvent is removed in vacuo
5. 5
   其他The crude product is purified by column chromatography (silica gel, PE/EtOAc 90/10 70/30)

实验过程

3.60 g (18.6 mmol) 5-bromo-2-chloropyrimidine, 4.80 g (55.8 mmol) cyclopropyl boronic acid, 13.8 g (65.1 mmol) K3PO4, 568 mg (2.03 mmol) tricyclohexylphosphine and 4 mL water are added to 80 mL toluene. The mixture is degassed thoroughly and charged with 627 mg (2.79 mmol) Pd(OAc)2. After degassing again the mixture is stirred at 100° C. over night, filtered and the solvent is removed in vacuo. The crude product is purified by column chromatography (silica gel, PE/EtOAc 90/10 70/30).

来源