Synthesis Of Nitrogen Heterocyclic Compounds With Expected Pharmaceutical Activity

Abstract

The original work of this thesis can be classified into two parts: Part (I): Multicomponent reactions, solvent-free synthesis of pyrido[2,3-d]pyrimidine-4(1H) dione derivatives and evaluation the pharmaceutical activity for new synthesized compounds. Part (II): Synthesis of some new substituted imidazoles carrying pyrazole moiety.

Part (I) In resumption of our work aiming to synthesize polyfunctional substituted heterocyclic compounds of potential biological activity, the synthesis of poly-functionalized 7-amino-5-(4-methoxyphenyl)-2,4-dioxo-1,2,3,4-tetrahydropyrido [2,3-d]pyrimidine-6-carbonitrile (1a) and 2-amino-4-(4-methoxyphenyl)-5-oxo-5H-dipyrido[1,2-a:3',2'-e]pyrimidine-3-carbonitrile (1b) was achieved via one-pot multicomponent reactions of the barbituric acid and/or 3H-pyrido [1,2-a]pyrimidine-2,4-dione, anisaldehyde, ammonium acetate and malononitrile or three-component reactions of barbituric acid and/or 3H-pyrido[1,2-a]pyrimidine-2,4-dione, arylidine of malononitrile and ammonium acetate in presencse of drops of triethylamine (TEA), under fusion at 150 oC (Scheme 1).