Reaktion #159652

Reaktionsgleichung

3-(3-fluorophenoxy)azetidine

triethylamine

2-Chloro-5-(trifluoromethyl)nicotinic acid

→

title compound

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

Lösungsmittel

methanol

Reaktionsbedingungen

Aufarbeitung

1. 1
   workup.ADDITIONwas added
2. 2
   Temperaturthe mixture was heated 10 min (2 cycles of 5 min each)
3. 3
   Sonstigeunder microwave irradiation at 150° C
4. 4
   SonstigeAfter solvent evaporation the residue
5. 5
   Sonstigewas purified by SPE-Si cartridge (25 g)
6. 6
   Wascheneluting with a mixture dichloromethane/methanol from 100/0 to 50/50
7. 7
   SonstigeCollected fraction
8. 8
   Sonstigeafter solvent evaporation

Vorschrift

To a mixture of 3-(3-fluorophenoxy)azetidine) (D50) (106.73 mg, 0.638 mmol) and triethylamine (0.11 ml, 0.798 mmol) in methanol (3 ml), 2-Chloro-5-(trifluoromethyl)nicotinic acid (120 mg, 0.532 mmol) was added and the mixture was heated 10 min (2 cycles of 5 min each) under microwave irradiation at 150° C. After solvent evaporation the residue was purified by SPE-Si cartridge (25 g) eluting with a mixture dichloromethane/methanol from 100/0 to 50/50. Collected fraction after solvent evaporation afforded the title compound (D121) (83 mg)

Quelle