New catalytic strategies for drug discovery

Overview & Synopsis

The central theme of my thesis is the development of new strategies for drug discovery, which is the interdisciplinary process involving chemistry, biology, and pharmacology These strategies have the potential to identify new medicines. The thesis is divided into three chapters.The first chapter is a critical review on enantioselective reactions involving nitriles that have been used in the synthesis of complex bioactive molecules.The second chapter describes my successful effort toward the development of a new multicomponent click-then-modify process for the preparation of peptide-drug conjugates featuring fluorescent linkers and the efficient synthesis of modifiable sequence defined oligomers.The third chapter of my thesis is about the development of a general strategy for the preparation of a wide range of of E- and Z-trisubstituted macrocyclic alkenes, which are important therapeutic agents. This can be synthesized through a stereoretentive catalytic macrocyclic ring-closing metathesis (MRCM) process. The method was applied to the synthesis of dolabelide C and fluvirucin.