Reaktion #6966

Reaktionsgleichung

3-hydroxy-4-fluorobenzoic acid

cyclopropylamine

triethylamine

HOBt

EDCI

→

3-hydroxy-4-fluoro-N-cyclopropylbenzamide

Ausbeute 61.5%

Lösungsmittel

DMF

water

Reaktionsbedingungen

Aufarbeitung

1. 1
   Extraktionextracted with ethyl acetate (3×20 mL)
2. 2
   WaschenThe extract was washed with water
3. 3
   Einengenconcentrated

Vorschrift

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%).

Quelle