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Abstract Substituted 3, I-benzoxazine-4-ones and 4(3-H)-quinazolinones exhibit a wide spectrum of pharmaceutical properties. Incorporation of such moieties in heterocyclic residues has lead to improved activities.(85-87) These findings prompted us, in this thesis, to synthesize 2-[( 4’-chloro-2’-methyl) phenoxymethyl]-6,8-dibromo-3,1- benzoxazin-4-one (2) for possible use, via its latent active functions, to produce a novel class of quinazolinone derivatives that are substituted with aryl, hetaryl or hetarylphenyl - isolated or fused - ring systems. The produced compounds might exhibit extended and/or improved biological and pharmacological activities. As will be shown in discussion part, most of the newly synthesized products contain a primary aromatic region (a), a carbonyl moiety (b), secondary aromatic moieties (c) and a polar lipophilic inhibitory function (d), all positioned at the appropriate distance for possible interaction with the complimentary binding sites in receptors of different biological cells and thus the new products might verify a very good conditions of pharmacophoric requirements for preparation of a more potent quinazoline-based pharmacologically active compounds. This present thesis comprises the following two parts: Part I: Which includes the use of 2-[(41-chloro methyl)phenoxymethyl}-6,8- dibromo-3,1-benzoxazin-4-one (2) as a key intermediate for synthesis of different multifunctional quinazoline derivatives (3-33).Part II: Which deals with the use of a group of quinazoline derivatives thata ccommodate one or two latent active methylene functions for usingin prior preparation of the corresponding a B-unsaturated quinazoline-based compounds. The latter products will be used - via the transition metal catalyzed technique - for synthesis of different Michael adducts. |