Executive Summary : | Multicomponent reactions are an interesting class of reactions that have become an independent domain of organic and synthetic medicinal chemistry. Tuning the reactants to different extents, this class of reactions has contributed to the synthesis of highly diverse heterocycles and highly functionalized complex molecular scaffolds in highly atom efficient ways. Specially isocyanide based multicomponent reactions(IMCRs) have contributed tremendously towards the construction of molecular libraries for drug discovery research, including applications in biomedical, pharmaceuticals and peptidomimetics. Among these transformations, four-component Ugi reaction and Post-Ugi modifications are quite noteworthy due to the incorporation of various functionalities of its components. Since its first report in 1959, various applications of Ugi reactions are reported for the synthesis of biologically active scaffolds. Howsoever, the development of enantioselective synthesis using post-IMCR reactions is still in the nascent stage. This proposal will focus on the development of a new synthetic pathway for the enantioselective synthesis of bioactive scaffolds, especially the development of organocatalytic transformations. Our principal goal is to develop new synthetic methodologies for the synthesis of drug-like molecules and alkaloid-mimicking molecular frameworks by asymmetric post-IMCR transformations. The developed methods will be employed to synthesize new chemical entities for the drug discovery and to identify novel and scalable process for bicalutamide drug. |