Reaktion #603205

Reaktionsgleichung

methyl 6-chloro-4-cyano-2-(1-methyl-1H-pyrazol-4-yl)nicotinate

(R)-2-amino-4-methylpentanamide

Water

→

title compound

Ausbeute 11.0%

(R)-Methyl 6-(1-amino-4-methyl-1-oxopentan-2-ylamino)-4-cyano-2-(1-methyl-1H-pyrazol-4-yl)nicotinate

Ausbeute 11.0%

Lösungsmittel

DMA

Reaktionsbedingungen

Aufarbeitung

1. 1
   Extraktionthe mixture was extracted with EtOAc
2. 2
   WaschenThe organic layers were washed with saturated aq NaHCO3, water, and brine
3. 3
   Trocknenwere dried over anhydrous Na2SO4
4. 4
   Filtrationfiltered
5. 5
   EinengenThe filtrate was concentrated under reduced pressure
6. 6
   SonstigeThe residue was purified by column chromatography (SiO2, EtOAc)

Vorschrift

A mixture of methyl 6-chloro-4-cyano-2-(1-methyl-1H-pyrazol-4-yl)nicotinate (82.9 mg, 0.300 mmol) and (R)-2-amino-4-methylpentanamide (39.0 mg, 0.300 mmol) in DMA (2 mL) was stirred at 150° C. for 12 h. Water was subsequently added and the mixture was extracted with EtOAc. The organic layers were washed with saturated aq NaHCO3, water, and brine, were dried over anhydrous Na2SO4, and filtered. The filtrate was concentrated under reduced pressure. The residue was purified by column chromatography (SiO2, EtOAc) to give the title compound as a yellow oil (11.7 mg, 11%).

Quelle