反応 #607863

反応方程式

6-aminopyridin-3-ol

1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxylic acid

EDCI

HOAT

→

title compound

収率 70.0%

N-(5-hydroxypyridin-2-yl)-1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide

収率 70.0%

溶媒

water

EtOAc

DMF

反応条件

後処理

1. 1
   温度cooled to rt
2. 2
   温度The mixture was cooled to 0° C.
3. 3
   workup.STIRRINGstirred overnight
4. 4
   ろ過The resulted solid was collected through filtration

実験手順

To a suspension of 6-aminopyridin-3-ol (330 mg, 3 mmol) and 1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxylic acid (710 mg, 306 mmol) in DMF (10 mL) was added EDCI (690 mg, 3.6 mmol) and HOAT (80 mg, 0.6 mmol). The reaction was stirred at 60° C. for 4 hours, then cooled to rt and diluted with water (100 mL) and EtOAc (2 mL). The mixture was cooled to 0° C. and stirred overnight. The resulted solid was collected through filtration to give title compound as a light brown solid (680 mg, 70%).

出典