Reaktion #159662

Reaktionsgleichung

2-(azetidin-3-yloxy)-5-fluoropyrimidine

triethylamine

2-chloro-5-(trifluoromethyl)nicotinic acid

→

title compound

Ausbeute 23.1%

2-(3-((5-fluoropyrimidin-2-yl)oxy)azetidin-1-yl)-5-(trifluoromethyl)nicotinic acid

Ausbeute 23.1%

Lösungsmittel

methanol

tetrahydrofuran

Reaktionsbedingungen

Aufarbeitung

1. 1
   workup.ADDITIONwas added
2. 2
   SonstigeAfter solvent evaporation the residue
3. 3
   Sonstigewas purified by SPE-Si cartridge (25 g)
4. 4
   Wascheneluting with a mixture dichloromethane/methanol from 95/5 to 80/20
5. 5
   SonstigeCollected fraction
6. 6
   Sonstigeafter solvent evaporation

Vorschrift

To a mixture of 2-(azetidin-3-yloxy)-5-fluoropyrimidine (D51) (108 mg, 0.638 mmol) and triethylamine (0.11 ml, 0.798 mmol) in methanol (1 ml) and tetrahydrofuran (2 ml), 2-chloro-5-(trifluoromethyl)nicotinic acid (120 mg, 0.532 mmol) was added and the mixture was heated 2 h at 80° C. After solvent evaporation the residue was purified by SPE-Si cartridge (25 g) eluting with a mixture dichloromethane/methanol from 95/5 to 80/20. Collected fraction after solvent evaporation afforded the title compound (D131) (44 mg)

Quelle