Executive Summary : | Innovations in chemical synthesis plays a crucial role in drug discovery and development. In particular, rapid and easy access to unattainable diversifications of medicinally relevant molecular scaffolds, accelerate and increase the success of pharmaceutical research. The biaryl moiety containing substructures are known to show dominant interactions with aromatic and hydrophobic residues with numerous binding sites. Consequently, the biaryl moiety is prevalent in many pharmaceuticals. Therefore, easy access to the construction of novel biaryl scaffolds with hitherto unprecedented functionalization patterns is highly desirable to generate novel NCEs for drug discovery research. The cyclic diaryliodonium salts have the potential to expand the chemical space for drug discovery by the direct construction of biaryl moiety with additional iodo functionality for further modification. However, the biaryltion of unactivated C(sp3)-H bond functionalization and bifunctionalization of cyclic diaryliodonium salts is still in its infancy. Thus, in this project, metal catalyzed bifunctionalization of cyclic diaryliodonium salts will be investigated to develop efficient protocols to access various biaryl derivatives decorated with multiple functionalizations. The developed synthetic protocols will be employed to prepare a library of privileged biaryl derivatives and subsequently will be evaluated for their biological activities particularly as antimicrobials. |