Peptide diversification: Pd-catalyzed derivatization of lead compounds in aqueous medium.

Drug discovery and development often involve the synthesis and evaluation of structural analogs of promising lead compounds.
The structural modification aims to increase biological potency, selectivity, water solubility, pharmacokinetics, therapeutic index and general ADMET properties. The most efficient way to realize this chemical modification requires a diversification reaction in a late stage of the synthesis route. Bio-orthogonal reactions, which allow the diversification or conjugation of protein or peptides, are of great interest. More specifically, reactions in an aqueous environment have proven to have great potential in the pharmaceutical industry.
This project envisages the use of peptides in the aqueous medium.