BIO ACTIVE SYNTHESIS OF 4-(HETERO AROMATIC ALDEHYDES)-6-METHYL-2-THIOXO-1, 2, 3, 4-TETRAHYDROPYRIMIDINE-5-CARBOXYLATE ESTERS USING METHANE SULFONIC ACID
B. V. Durgarao, N. Srinivas Rao, V. Kalpana, V. Narasing Rao and Dr. N. Krishnarao*
ABSTRACT
As a part of our research in the synthesis of pyrimidine derivatives containing biological activities, some new tetrahydropyrimidine derivatives (1-6) were synthesized. The present study, the synthesis of some novel Biginelli-type pyrimidine is reported. The prepared compounds are ethanone derivatives of 6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidines with a simple heteroarylaldehydes group at C-4 position of the pyrimidine ring. These compounds can be obtained the reaction of heteroaromatic aldehydes (1.2 mmol), acetyl acetone (1mmol), thiourea(1mmol) in the presence of Methanesulfonic acid at1200C conditions. All the compounds were examined by advanced spectroscopic data (1H NMR, 13C NMR& LCMS) and the structural determination was calculated by elemental analysis. In addition to the all newly synthesized compounds were screened by their microbial activity .The antibacterial activity of some synthesized compounds was investigated against Staphylococcus aureus, Esherichiacoli, S.typhi, BacillusSubstills), Some of these compounds such as 4d,4e and exhibited a good to significant antibacterial activity.
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