Design of novel methodologies for the synthesis of heterocycles
Keywords:
chemical synthesis, heterocycles, organocatalysis, photocatalysis, multicomponent reactionsAbstract
Introduction: The synthesis of heterocyclic compounds with potential biological activity is one of the main strategies for drug discovery and development.
Objective: To develop novel methodologies for the stereo and regioselective, multicomponent and catalytic synthesis of heterocyclic scaffolds considered as privileged for medicinal chemistry applications.
Methods: The research carried out combines various modern methods of organic synthesis that comprises the following approaches. The use of organocatalysis for the asymmetric functionalization of carbonyl groups, followed by stereoselective multicomponent reactions for obtaining heterocyclic analogues of natural products. Heterocyclization reactions catalyzed by rhodium and ruthenium for the derivatization of peptidic substrates, achieving the synthesis of chimeric molecules having fused heterocycles and heterocycle-peptide hybrid skeletons. The photocatalytic functionalization of heterocyclic skeletons for the generation of structural diversity in nitrogenated molecules of biological relevance. Additionally, the use of computational chemistry tools allowed to explain the regioselectivity of the reactions developed.
Conclusions: The reactions catalyzed by small organic molecules or transition metals and their combination with multicomponent reactions are powerful synthetic tools for producing heterocyclic compounds in high chemical efficiency, atomic economy and with generation of great structural diversity.
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