Реакция #48493

Уравнение реакции

3-((6-chloronaphthalen-2-yl)sulfonyl)propinoic acid

HOBt

WSC

1-(piperidin-4-yl)-2-pyrrolidinone

→

title compound

Выход 39.0%

1-(1-{3-[(6-Chloronaphthalen-2-yl)sulfonyl]propanoyl}piperidin-4-yl)pyrrolidin-2-one

Выход 39.0%

Растворители

DMF

triethylamine

Условия реакции

Обработка

1. 1
   КонцентрированиеThe reaction mixture was concentrated under reduced pressure
2. 2
   workup.ADDITIONdiluted with ethyl acetate
3. 3
   ДругоеThe organic layer was separated
4. 4
   Сушкаdried over anhydrous sodium sulfate
5. 5
   Концентрированиеconcentrated under reduced pressure
6. 6
   ДругоеThe residue was purified by basic silica gel column chromatography (ethyl acetate to ethyl acetate/methanol 10/1)

Методика

After 3-((6-chloronaphthalen-2-yl)sulfonyl)propinoic acid (0.30 g), HOBt (0.23 g) and WSC (0.29 g) were dissolved in DMF (10 mL), 1-(piperidin-4-yl)-2-pyrrolidinone (0.17 g) and triethylamine (0.10 g) were added thereto, and the mixture was stirred at room temperature for 15 hours. The reaction mixture was concentrated under reduced pressure, and diluted with ethyl acetate and an aqueous sodium bicarbonate solution. The organic layer was separated, dried over anhydrous sodium sulfate, and concentrated under reduced pressure. The residue was purified by basic silica gel column chromatography (ethyl acetate to ethyl acetate/methanol 10/1) to obtain the title compound (0.17 g, 39%) as a colorless powder.

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