Synthesis and bioassay studies of 7-substituted pyrido[2,3-d]pyrimidines

ABSTRACT:

4-Aminopyrimidine-5-carbaldehyde 1 underwent facile condensation with various aromatic ketone derivatives in the presence of K2CO3 and small catalytic amount of KI in acetone was afforded corresponding 7-Substituted pyrido[2,3-d]pyrimidine derivatives 3a-j. Their chemical structures were characterized using IR, H1 NMR and Mass spectral studies. All the above compounds were screened for anti-microbial activity, anti-oxidant activity and their bioassay showed them to possess significant antimicrobial activity and anti-oxidant activity.

Introduction:

 For small organic molecules, simple nitrogen-containing heterocycles receive a large amount of attention in the literature, of these heterocycles, the synthesis, reactions and biological activities of pyridine containing molecules stands as an ever expanding area of research in hetero aromatic chemistry. pyrido[2,3-d]pyrimidine heterocycles have received much less attention in the literature, in spite of their structural relationship to pyridines. Interest in pyrido[2,3-d]pyrimidine derivatives has increased dramatically in recent years, based upon a diverse range of biological properties as antitumour, antibacterial, anti-inflammatory, insecticidal agents, diuretics properties and activity against platelet aggregation. To continue our interest in the synthesis of simple nitrogen-containing heterocycles. We set out to develop a new method for the synthesis of highly-functionalised, pyrido [2,3-d] pyrimidine heterocycles. Central to our approach was the need to develop a novel method, using readily available starting materials and simple experimental procedures and very good yields. This paper describes a new and highly efficient method for the preparation of pyrido[2,3-d]pyrimidines that exhibits all of these features.

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