반응 #66531

반응 방정식

N-(3-chloro-4-(piperazin-1-yl)phenyl)picolinamide

propionic acid

EDCI.HCl

Et3N

hydroxybenzotriazole

→

N-(3-chloro-4-(4-propionylpiperazin-1-yl)phenyl)picolinamide

수율 73.7%

용매

DCM

반응 조건

후처리

1. 1
   기타The solution was quenched with water
2. 2
   추출The aqueous phase was extracted with DCM
3. 3
   세척The organic phase was washed with brine
4. 4
   건조was dried over Na2SO4
5. 5
   여과was filtered
6. 6
   농축was concentrated under reduced pressure
7. 7
   기타The solid was triturated with water and finally with iPr2O

실험 절차

According to Scheme 5 Step 5 Method A: A solution of N-(3-chloro-4-(piperazin-1-yl)phenyl)picolinamide (0.19 mmol, 60 mg), propionic acid (0.19 mmol, 14 μL), EDCI.HCl (0.28 mmol, 54 mg), Et3N (0.38 mmol, 53 μL) and of hydroxybenzotriazole (0.21 mmol, 32 mg) in DCM (5 mL) was stirred at room temperature for 1 day. The solution was quenched with water. The aqueous phase was extracted with DCM. The organic phase was washed with brine, was dried over Na2SO4, was filtered and was concentrated under reduced pressure. The solid was triturated with water and finally with iPr2O to afford N-(3-chloro-4-(4-propionylpiperazin-1-yl)phenyl)picolinamide (0.14 mmol, 51 mg, 72%) as a yellow solid.

출처