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SYNTHESIS OF BIOLOGICALLY ACTIVITY HYBRID DIAZINE - POLYPHENOLS DERIVATIVES USING ECOLOGICALLY FRIENDLY METHODS
Abstract
We present herein a thoroughly study regarding the synthesis, structure and biological activity of some hybrid diazine - polyphenols derivatives. The synthesis was performed under conventional thermal heating and microwave irradiation, by using a straight and efficient method: a N-alkylation reaction of diazine (pyridazine or phthalazine) with reactive halogenated derivatives. The structure of the hybrids was proven by elemental and spectral analysis. Under MW irradiation, the N-alkylation reaction of diazine have some undeniable advantages in terms of higher yields, a substantially decrease of the reaction times (from hours to minutes) and of the amount of used solvents (4 folds less), a remarkable acceleration of reaction. As a result, the N-alkylation reaction of diazine heterocycles under MW irradiation could be considered as environmentally friendly. The hybrid diazine - polyphenols derivatives have a very good antimicrobial activity against both fungus and Gram-positive and Gram-negative germs. The anticancer activity proved to be moderate.
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