反应详情

3-methyl-6-[2-(p-toluenesulfonyloxy)ethyl]oxazolo[4,5-b]pyridin-2(3-one of Preparation 15 (210 mg, 1.2 mmol) is dissolved in 1,4-dioxane (8 ml). N-phenyl-piperazine (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##

1. customAfter the solvent has been evaporated off under reduced pressure
2. extractionExtraction
3. dry with materialthe organic phase is dried over magnesium sulfate
4. filtrationfiltered
5. customthe solvent is evaporated off
6. customThe title product is purified by chromatography on silica gel (eluant: dichloromethane/methanol: 95/5)
7. customThe yield obtained