Reaktion #45290

Reaktionsgleichung

3-(2-difluoromethoxyphenylmethanesulfonyl)-2(R)-[2,2,2-trifluoro-1(RS)-(4-fluorophenyl)ethylamino]propionic acid

1-aminocyclopropanecarbonitrile hydrochloride

HATU

DIPEA

→

title compound

Ausbeute 70.0%

N-(1-cyanocyclopropyl)-3-(2-difluoromethoxyphenylmethanesulfonyl)-2(R)-[2,2,2-trifluoro-1 (s)-(4-fluorophenyl)ethylamino]propionamide

Ausbeute 70.0%

Lösungsmittel

DMF

Reaktionsbedingungen

Aufarbeitung

1. 1
   Extraktionthe reaction mixture was extracted with ethyl acetate (100 mL)
2. 2
   Waschenwashed with satured NaHCO3 and brine
3. 3
   TrocknenAfter drying with MgSO4
4. 4
   Sonstigethe solvent was removed
5. 5
   Sonstigethe residue was purified by column chromatograph

Vorschrift

To a solution of 3-(2-difluoromethoxyphenylmethanesulfonyl)-2(R)-[2,2,2-trifluoro-1(RS)-(4-fluorophenyl)ethylamino]propionic acid (157 mg, 0.325 mmol) in DMF (5 mL) was added 1-aminocyclopropanecarbonitrile hydrochloride (46.4 mg, 0.39 mmol), HATU (186.3 mg, 0.49 mmol) and DIPEA (63.2 mg, 0.49 mmol). After 1 h, the reaction mixture was extracted with ethyl acetate (100 mL) and washed with satured NaHCO3 and brine. After drying with MgSO4, the solvent was removed and the residue was purified by column chromatograph yield the title compound (125 mg).

Quelle