Reaktion #1533338

Reaktionsgleichung

5-[4-(Trifluoromethyl)phenyl]isoxazole-4-carboxylic acid

o-(benzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium tetrafluoroborate

pyridine

2-pyrrolidin-3-yl-pyrazine trihydrochloride

→

title compound

Ausbeute 55.8%

2-[1-({5-[4-(Trifluoromethyl)phenyl]isoxazol-4-yl}carbonyl)pyrrolidin-3-yl]pyrazine

Ausbeute 55.8%

Lösungsmittel

acetonitrile

Reaktionsbedingungen

Aufarbeitung

1. 1
   SonstigeThe residue was purified on reversed phase HPLC

Vorschrift

5-[4-(Trifluoromethyl)phenyl]isoxazole-4-carboxylic acid (30 mg, 0.12 mmol) was dissolved in acetonitrile (1.5 mL) followed by the addition of o-(benzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium tetrafluoroborate (TBTU) (52 mg, 0.16 mmol), pyridine (60 μL, 0.72 mmol) and 2-pyrrolidin-3-yl-pyrazine trihydrochloride (36 mg, 0.14 mmol), and stirred at 60° C. for 30 min. The residue was purified on reversed phase HPLC to yield the title compound (26 mg). HRMS (ESI, pos. ion) m/z calcd for C19H15F3N4O2: 388.1147, found 388.1152.

Quelle