Reaktion #2474640

Reaktionsgleichung

4-bromo-6,6a-dihydro-1aH-indeno[1,2-b]oxirene

tert-butyl 4-methyl-4-[(3S)-3-methylpiperazin-1-yl]piperidine-1-carboxylate

→

desired compound

Ausbeute 49.4%

tert-Butyl 4-{(3S)-4-[(1R,2R)-5-Bromo-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-3-methylpiperazin-1-yl}-4-methylpiperidine-1-carboxylate

Ausbeute 49.4%

Lösungsmittel

ethanol

Reaktionsbedingungen

Aufarbeitung

1. 1
   TemperaturThe reaction mixture was heated
2. 2
   Temperaturto reflux overnight
3. 3
   TemperaturAfter cooling down
4. 4
   Sonstigethe mixture was evaporated under reduced pressure
5. 5
   SonstigePurification on silica gel with 50% ethyl acetate (1% NH4OH) and hexane
6. 6
   Sonstigeafforded the

Vorschrift

To a solution of 4-bromo-6,6a-dihydro-1aH-indeno[1,2-b]oxirene (247.9 mg, 1.1746 mmol) in ethanol (10.00 mL) was added tert-butyl 4-methyl-4-[(3S)-3-methylpiperazin-1-yl]piperidine-1-carboxylate (349.36 mg, 1.1746 mmol). The reaction mixture was heated to reflux overnight. After cooling down, the mixture was evaporated under reduced pressure. Purification on silica gel with 50% ethyl acetate (1% NH4OH) and hexane afforded the fast moving product as the desired compound (295 mg; 49.4%).

Quelle