تفاعل #6966

معادلة التفاعل

3-hydroxy-4-fluorobenzoic acid

cyclopropylamine

triethylamine

HOBt

EDCI

→

3-hydroxy-4-fluoro-N-cyclopropylbenzamide

المردود 61.5%

المذيبات

DMF

water

ظروف التفاعل

المعالجة

1. 1
   استخلاصextracted with ethyl acetate (3×20 mL)
2. 2
   غسيلThe extract was washed with water
3. 3
   تركيزconcentrated

الإجراء التجريبي

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%).

المصدر