反应 #41631

反应方程式

1-(t-butoxycarbonyl)pyrrole-2-boronic acid

sodium carbonate

water

4-bromo-3-fluoro-phenylamine

→

compound

t-butyl 2-(4-amino-2-fluoro-phenyl)-pyrrole-1-carboxylate

溶剂

dimethoxyethane

反应条件

后处理

1. 1
   其他the reaction liquid
2. 2
   温度After cooled
3. 3
   其他the reaction liquid
4. 4
   过滤was filtered through Celite
5. 5
   workup.ADDITIONthe filtrate was diluted with ethyl acetate
6. 6
   洗涤washed with water and saturated saline in order
7. 7
   干燥dried with anhydrous magnesium sulfate
8. 8
   其他The solvent was evaporated away under reduced pressure
9. 9
   其他the resulting residue was purified through silica gel column chromatography (developing solvent: hexane/ethyl acetate=2/1)

实验过程

1.6 g of 1-(t-butoxycarbonyl)pyrrole-2-boronic acid, 200 mg of tetrakistriphenylphosphine palladium, 5 ml of aqueous saturated sodium carbonate solution and 5 ml of water were added in order to a dimethoxyethane (10 ml) solution of 1 g of 4-bromo-3-fluoro-phenylamine, and the reaction liquid was stirred in a nitrogen atmosphere at 70° C. for 3 hours. After cooled, the reaction liquid was filtered through Celite, and the filtrate was diluted with ethyl acetate, washed with water and saturated saline in order, and dried with anhydrous magnesium sulfate. The solvent was evaporated away under reduced pressure, and the resulting residue was purified through silica gel column chromatography (developing solvent: hexane/ethyl acetate=2/1) to obtain the entitled compound as a pale brown solid.

来源