Paper Title
EFFECT OF THE NATURE OF MALONIC ACID DERIVATIVES ON THE SYNTHESIS REACTION OF PYRIMIDINIUM BÉTAINES, CHARACTERIZATION AND BIOLOGICAL ACTIVITY

Abstract
Abstract - Malonic acid derivatives are widely used in chemistry as organic synthesis intermediates. However, the study of the synthesis reaction of betaines with a pyrimidine ring has shown that the nature of the malonic esters used as reactant has a considerable effect on the reaction conditions of these compounds.In this work, we were interested in the study of the reactivity of some malonic esters, by their condensation with amine derivatives for the synthesis of betaines containing a pyrimidine ring. The study showed that in the case of the reaction of malonic esters not very active such as alkyl malonates with 2-aminopyridine or amidine derivatives, extreme conditions were used that is heating the mixture at high temperature for several hours. Substituting these commercially available esters with bistrichlorophenyl esters of malonic acid as more reactive ester, the reaction time is reduced, but high temperature heating is still required. To further increase the reactivity of the malonic esters, bispentachlorophenyl esters of malonic acid were used. Due to the presence of 10 chlorine atoms in their structure, these latter react with 2-aminopyridine or amidines derivatives under mild conditions and the reaction takes place in a few minutes. Considering the chemical activity of malonic acid bispentachlorophenyl ester, we synthesized and evaluated the biological activity of this compound. The results showed that this organochlorine compound revealed significant antimicrobial activity against the target germs: Bacillus subtilus, Salmonella enterica Mucor ramannianus and Candida albicans, These results suggest that malonic acid bispentachlorophenyl ester could be useful for the development of new antimicrobial drugs and might be used in many diseases Keywords: Malonic acid derivatives, Synthesis, Characterization, Antimicrobial activity.