Реакция #11980

Уравнение реакции

triethylamine

Benzotriazol-1-yloxy-tris(dimethylamino)-phosphonium hexafluorophosphate

7-amino-5-(3,4-dichloro-phenyl)-pyrazolo[1,5-a]pyrimidine-2-carboxylic acid

benzylamine

→

7-amino-5-(3,4-dichloro-phenyl)-pyrazolo[1,5-a]pyrimidine-2-carboxylic acid benzylamide

Выход 55.0%

Растворители

ethyl ether

tetrahydrofuran

Условия реакции

Обработка

1. 1
   Промывкаwashed with a saturated aqueous solution of sodium bicarbonate (10 mL)
2. 2
   ДругоеThe organic layer was collected
3. 3
   Концентрированиеconcentrated under reduced pressure
4. 4
   Другоеthe crude product was purified by column chromatography

Методика

Benzotriazol-1-yloxy-tris(dimethylamino)-phosphonium hexafluorophosphate (BOP) (0.081 g, 0.184 mmol) was added to a suspension of 7-amino-5-(3,4-dichloro-phenyl)-pyrazolo[1,5-a]pyrimidine-2-carboxylic acid (0.050 g, 0.154 mmol) and benzylamine (0.034 mL, 0.308 mmol) in tetrahydrofuran (5 ml) containing triethylamine (0.064 mL, 0.462 mmol). The reaction mixture was stirred overnight at room temperature, diluted with ethyl ether (5 mL) and washed with a saturated aqueous solution of sodium bicarbonate (10 mL). The organic layer was collected, concentrated under reduced pressure and the crude product was purified by column chromatography to give 7-amino-5-(3,4-dichloro-phenyl)-pyrazolo[1,5-a]pyrimidine-2-carboxylic acid benzylamide (0.026 g, 55%).

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