Reacción #95354

ord-609aaef785044093b5b2a20a3ab02518

Ecuación de reacción

Cl.O=C1Nc2ccccc2CN1C1CCNCC1
4-[3,4-dihydro-2(1H)-quinazolinon-3-yl]-piperidine mono-hydrochloride
O=C(CBr)c1ccc(Cl)cc1
α-bromo-p-chloroacetophenone
CCN(CC)CC
triethylamine
O=C(CN1CCC(N2Cc3ccccc3NC2=O)CC1)c1ccc(Cl)cc1
desired product
Rendimiento 56.0%
O=C(CN1CCC(N2Cc3ccccc3NC2=O)CC1)c1ccc(Cl)cc1
1-(4-Chlorobenzoylmethyl)-4-[3,4-dihydro-2(1H)-quinazolinon-3-yl]-piperidine
Rendimiento 56.0%

Disolventes

Condiciones de reacción

Condiciones detalladas
See reaction.notes.procedure_details.

Tratamiento posterior

  1. 1
    OtroThe white crystals deposited are separated by filtration
  2. 2
    Lavadosuccessively washed with methanol and water
  3. 3
    Otrodried
  4. 4
    Otroto obtain 5.17 g of a crude product
  5. 5
    OtroThe crude product is recrystallized from a mixed solvent of chloroform and ethanol

Procedimiento

In this example, 4.0 g of 4-[3,4-dihydro-2(1H)-quinazolinon-3-yl]-piperidine mono-hydrochloride, 3.5 g of α-bromo-p-chloroacetophenone, 4.2 ml of triethylamine and 60 ml of methanol are mixed and stirred at room temperature overnight. The white crystals deposited are separated by filtration, successively washed with methanol and water and dried to obtain 5.17 g of a crude product. The crude product is recrystallized from a mixed solvent of chloroform and ethanol to obtain 3.21 g of the desired product.

Fuente

DOI: 10.6084/m9.figshare.5104873.v1Patente: US04344948uspto-grants-1982_08