Reaktion #81453

Reaktionsgleichung

3-methyl-6-[2-(p-toluenesulfonyloxy)ethyl]oxazolo[4,5-b]pyridin-2(3H)-one

N-phenylpiperazine

triethylamine

→

3-METHYL-6-[2-(4-PHENYLPIPERAZIN-1-YL)ETH-1-YL]OXAZOLO[4,5-b]PYRIDIN-2(3H)-ONE

Lösungsmittel

1,4-dioxane

Reaktionsbedingungen

Aufarbeitung

1. 1
   SonstigeAfter the solvent has been evaporated off under reduced pressure
2. 2
   ExtraktionExtraction
3. 3
   Trocknenthe organic phase is dried over magnesium sulfate
4. 4
   Filtrationfiltered
5. 5
   Sonstigethe solvent is evaporated off
6. 6
   SonstigeThe title product is purified by chromatography on silica gel (eluant: dichloromethane/methanol: 95/5)
7. 7
   SonstigeThe yield obtained

Vorschrift

3-methyl-6-[2-(p-toluenesulfonyloxy)ethyl]oxazolo[4,5-b]pyridin-2(3H)-one of Preparation 15 (210 mg, 1.2 mmol) is dissolved in 1,4-dioxane (8 ml). N-phenylpiperazine (0.10 ml, 1.38 mmol) and triethylamine (0.18 ml, 1.3 mmol) are added in succession to the reaction mixture. Stirring is maintained at room temperature for 24 hours. After the solvent has been evaporated off under reduced pressure, the residue is taken up in water. Extraction is carried out with dichloromethane and the organic phase is dried over magnesium sulfate and filtered, and then the solvent is evaporated off. The title product is purified by chromatography on silica gel (eluant: dichloromethane/methanol: 95/5). The yield obtained is 91%. ##STR66##

Quelle