AgOTf‑CATALYZED SYNTHESIS AND ANTIMICROBIAL EVALUATION OF NITROGEN/SULFUR‑BEARING THIADIAZOLO[3,2‑A] PYRIMIDINES
In this study, AgOTf was used as a catalyst to synthesize N, S-thiadiazolo[3,2-a] pyrimidine derivatives, alkyl &aryl Chiral aldoses, and pyrimidine-based amines. A mild reaction procedure involving a Lewis Acid activationof an Aldehyde, followed by a cyclocondensation to produce fused heterocycles in pure analytical formwith simpleisolation procedures, was employed. Several aryl groups were introduced to install diverse functionalities, and thesefunctionalities were produced in appreciable yields, indicating the robustness of the synthetic procedure andtheefficiency of the operation. The designed moiety of the currently prepared derivatives has been analyzedviaestablished methods (M.p, NMR, LC-MS, and other routine analytical methods), and appropriate antimicrobial activity against representative G+, G- bacteria and selected fungi has been demonstrated. The fact that multiplederivatives have shown significant activity suggests that the biological response can be tuned by varying substituentson the thiadiazolo[3,2-a] pyrimidine scaffold. This work will contribute to the ongoing search for newantibacterial leads and demonstrate the potential of AgOTf-catalyzed multicomponent reactions to rapidly generate bioactive N/SCompounds, consistent with Sustainable Development Goal 3 in Good Health & Well-Being.
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