Collect. Czech. Chem. Commun. 1991, 56, 2373-2381

Synthesis and analgetic efficiency of some oxy and oxo derivatives of 4(3H)-quinazolinone

Ludmila Fišnerová, Bohumila Brunová, Zuzana Kocfeldová, Jana Tíkalová, Eva Maturová and Jaroslava Grimová

Research Institute of Pharmacy and Biochemistry, 130 60 Prague 3


A series of 3-substituted 4(3H)-quinazolinone derivatives have been prepared by alkylation of 4(3H)-quinazolinone with halogenoethers, halogenoketones, and Mannich bases, and the products have been tested for analgetic effects.The most interesting representatives of the oxy and oxo derivatives are 3-[2-(2’,4’-difluoro-4-biphenylyloxy)ethyl]-4(3H)-quinazolinone (Ib) and 3-[2-oxo-2-(4-biphenylyl)ethyl]-4(3H)-quinazolinone (IIi), respectively. Among the group of oxy derivatives also the 2-methylderivative Ig has been prepared, viz. by alkylation of 2’,4’-difluoro-4-hydroxybiphenyl with 2-methyl-3-(2-chloroethyl)-4(3H)-quinazolinone; the activity of Ig is lower than that of Ib.