반응 #332184

반응 방정식

Trimethylsilyl cyanide

43a

4-(4-aminophenyl)-piperazine-1-carboxylic acid tert-butyl ester

cyclobutanone

sodium sulfate

→

43b

수율 84.0%

4-[4-(1-cyanocyclobutylamino)phenyl]-piperazine-1-carboxylic acid tert-butyl ester

수율 84.0%

용매

dichloromethane

acetone

dichloromethane

반응 조건

후처리

1. 1
   여과After filtration
2. 2
   농축the medium was concentrated under vacuum
3. 3
   기타to obtain a brown liquid which

실험 절차

Trimethylsilyl cyanide (0.3 g, 3 mmol) was added dropwise to a mixture of 43a (0.415 g, 1.5 mmol), cyclobutanone (0.21 g, 3 mmol) and sodium sulfate (1 g) in dichloromethane (5 ml). The mixture was stirred for 15 hours. After filtration to eliminate sodium sulfate, the medium was concentrated under vacuum to obtain a brown liquid which was subjected to chromatography (dichloromethane:acetone, 75:25) to yield 43b (0.448 g, 1.26 mmol, 84%) as a yellow solid.

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