反応 #6966

反応方程式

3-hydroxy-4-fluorobenzoic acid

cyclopropylamine

triethylamine

HOBt

EDCI

→

3-hydroxy-4-fluoro-N-cyclopropylbenzamide

収率 61.5%

溶媒

DMF

water

反応条件

後処理

1. 1
   抽出extracted with ethyl acetate (3×20 mL)
2. 2
   洗浄The extract was washed with water
3. 3
   濃縮concentrated

実験手順

To a mixture of 3-hydroxy-4-fluorobenzoic acid (1.56 g, 10 mmol), cyclopropylamine (0.6 g, 10.5 mmol), triethylamine (1.02 g, 10 mmol) and HOBt (0.3 g, 2 mol) in DMF (10 mL) was added EDCI (2.0 g, 10.5 mmol) at RT. The mixture was stirred at RT overnight. The mixture was diluted with water and extracted with ethyl acetate (3×20 mL). The extract was washed with water and concentrated to afford 3-hydroxy-4-fluoro-N-cyclopropylbenzamide as a solid (1.2 g, 61.5%).

出典