반응 #8376

반응 방정식

5-pyridin-2-yl-4-quinolin-4-yl 2H-pyrazol-3-ol

ethylene glycol

tri-n-butylphosphine

1,1′-(azodicarbonyl)dipiperidine

→

title compound

수율 74.9%

4-(6-Pyridin-2-yl-2,3-dihydro-pyrazolo[5,1-b]oxazol-7-yl)-quinoline

수율 74.9%

용매

tetrahydrofuran

반응 조건

후처리

1. 1
   온도The solution is heated
2. 2
   온도at reflux for 5 h
3. 3
   온도cooled
4. 4
   여과filtered through an SCX cartridge
5. 5
   기타The residue is chromatographed on SiO2 (15:1 dichloromethane:methanol)

실험 절차

To a solution of 5-pyridin-2-yl-4-quinolin-4-yl 2H-pyrazol-3-ol (50 mg, 0.17 mmol), ethylene glycol (15 mg, 0.24 mmol) and tri-n-butylphosphine (100 mg, 0.50 mmol) in tetrahydrofuran (15 mL) is added 1,1′-(azodicarbonyl)dipiperidine (120 mg, 0.48 mmol). The solution is heated at reflux for 5 h, cooled, and filtered through an SCX cartridge. The residue is chromatographed on SiO2 (15:1 dichloromethane:methanol). The product residue is converted to the disoxylate salt to give the title compound 40 mg (46%).

출처