Реакция #6966

Уравнение реакции

3-hydroxy-4-fluorobenzoic acid

cyclopropylamine

triethylamine

HOBt

EDCI

→

3-hydroxy-4-fluoro-N-cyclopropylbenzamide

Выход 61.5%

Растворители

DMF

water

Условия реакции

Обработка

1. 1
   Экстракцияextracted with ethyl acetate (3×20 mL)
2. 2
   ПромывкаThe extract was washed with water
3. 3
   Концентрированиеconcentrated

Методика

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%).

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