반응 #1932042

반응 방정식

2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-pyrazolo[3,4-f]quinoline-7-carboxylic acid

thiomorpholine-1,1-dioxide hydrochloride

DIEA

HATU

→

product

수율 76.2%

2-chloro-4-(3-cyclopentyl-7-(1,1-dioxidothiomorpholine-4-carbonyl)-3,3a,4,5-tetrahydro-2h-pyrazolo[3,4-f]quinolin-2-yl)benzonitrile

수율 76.2%

용매

dichloromethane

DMF

반응 조건

후처리

1. 1
   농축was concentrated under reduced pressure
2. 2
   workup.ADDITIONWater was added to the residue
3. 3
   여과The mixture was filtered
4. 4
   기타to produce a crude yellow solid, which
5. 5
   세척was washed with methanol

실험 절차

In a dried reaction flask, 2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-pyrazolo[3,4-f]quinoline-7-carboxylic acid (0.421 g, 1.0 mmol), thiomorpholine-1,1-dioxide hydrochloride (0.223 g, 1.3 mmol), DIEA (0.26 mL, 1.49 mmol), and HATU (0.418 g, 1.1 mmol) were added to a mixed solvent of DMF (4 mL) and dichloromethane (8 mL). The mixture was stirred at room temperature for 1.5 hr and was concentrated under reduced pressure. Water was added to the residue. The mixture was filtered to produce a crude yellow solid, which was washed with methanol to obtain a purified product (0.410 g) in 76.2% yield.

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