Diversity-Oriented Synthesis of new chemical entities exploiting Carbonyl-Coupling reactions.

The research of New Molecular Entities (NME) with a biological activity is one of the most important topics in modern Drug Discovery, because after an impressive growth at the end of the last Century, the number of NME launched on the drug-market dramatically decreased in recent years. The application of Diversity-Oriented-Synthesis (DOS) has been placed as a new paradigm for the revival of drug discovery, and has received great interest in the biomedical field during last years. DOS consists of generating structurally diverse compounds from a complexity generating reaction followed by cyclization steps and appendage diversity .One of the most employed strategy uses in this field was the Build/Couple/Pair (B/C/P) approach, it is a synthetic strategy uses for the generation of the molecular diversity on three different step. In this type of approach the "Couple" step represents the core of the strategy; indeed based on the chemical approach used in this phase suitable the building blocks are required, and consequently the functional groups available for the pair step. In this work I studied several reactions for their application as couple reaction in B/C/P strategies.