Reaktion #83224

Reaktionsgleichung

5-amino-3-(4-fluorophenyl)-4-(pyridin-4-yl)pyrazole

methyl acrylate

pyridine

→

2-(4-fluorophenyl)-5-oxo-3-(pyridin-4-yl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine

Lösungsmittel

water

Reaktionsbedingungen

Aufarbeitung

1. 1
   Temperaturwas refluxed for 8 hours
2. 2
   TemperaturThe mixture was cooled
3. 3
   Einengenconcentrated in vacuo
4. 4
   workup.DISSOLUTIONThe residue was dissolved in a mixture of acetic acid (10 ml) and concentrated hydrochloric acid (1.5 ml)
5. 5
   TemperaturThe solution was refluxed for 2 hours
6. 6
   Temperaturcooled
7. 7
   SonstigeThe separated solid was collected
8. 8
   Waschenwashed with water
9. 9
   Sonstigedried

Vorschrift

A mixture of 5-amino-3-(4-fluorophenyl)-4-(pyridin-4-yl)pyrazole (1.016 g), methyl acrylate (10 ml), pyridine (20 ml) and water (5 ml) was refluxed for 8 hours. The mixture was cooled and concentrated in vacuo. The residue was dissolved in a mixture of acetic acid (10 ml) and concentrated hydrochloric acid (1.5 ml). The solution was refluxed for 2 hours, cooled and neutralized with an aqueous saturated sodium bicarbonate solution. The separated solid was collected, washed with water and dried to give 2-(4-fluorophenyl)-5-oxo-3-(pyridin-4-yl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine (750 mg).

Quelle