Reacción #6966

Ecuación de reacción

3-hydroxy-4-fluorobenzoic acid

cyclopropylamine

triethylamine

HOBt

EDCI

→

3-hydroxy-4-fluoro-N-cyclopropylbenzamide

Rendimiento 61.5%

Disolventes

DMF

water

Condiciones de reacción

Tratamiento posterior

1. 1
   Extracciónextracted with ethyl acetate (3×20 mL)
2. 2
   LavadoThe extract was washed with water
3. 3
   Concentraciónconcentrated

Procedimiento

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%).

Fuente