Reaktion #1704887

Reaktionsgleichung

4-[3-(1-methyl-6-oxo-1,6-dihydro-pyridin-3-yl)-3-oxo-1-o-tolyl-propyl]-benzoic acid

morpholine

benzotriazol-1-yloxytris(dimethylamino) phosphonium hexafluorophosphate

N-ethyldiisopropylamine

→

title compound

Ausbeute 105.6%

1-Methyl-5-{3-[4-(morpholine-4-carbonyl)-phenyl]-3-o-tolyl-propionyl}-1H-pyridin-2-one

Ausbeute 105.6%

Lösungsmittel

tetrahydrofuran

Reaktionsbedingungen

Aufarbeitung

1. 1
   EinengenThe mixture was concentrated to dryness
2. 2
   SonstigeThe product was purified by chromatography (SiO2, dichloromethane/methanol 1:0 to 9:1)

Vorschrift

A mixture 4-[3-(1-methyl-6-oxo-1,6-dihydro-pyridin-3-yl)-3-oxo-1-o-tolyl-propyl]-benzoic acid (60 mg), morpholine (17 mg), benzotriazol-1-yloxytris(dimethylamino) phosphonium hexafluorophosphate (108 mg, BOP reagent) and N-ethyldiisopropylamine (62 mg) in tetrahydrofuran (0.6 ml) was stirred overnight at room temperature. The mixture was concentrated to dryness. The product was purified by chromatography (SiO2, dichloromethane/methanol 1:0 to 9:1) to give the title compound (75 mg) as a colorless foam, MS (ESI+): m/z=445.4 [M+H]+.

Quelle