Application of Barluenga Boronic Coupling (BBC) to the Parallel Synthesis of Drug-like and Drug Fragment-like Molecules

摘要

Library and array synthesis has proven an invaluable tool for nneclicinal chemists to quickly assess key structure-activity relationships against a biological target. The main requirements for the adoption of a given synthetic protocol are: 1) the availability of a diverse set of monomers (building blocks), 2) the reaction should be adapted to the preparation of drug-like molecules and thus should tolerate a wide range of functional groups, and 3) the process should ideally be air- and moisture-tolerant. As a consequence, the protocols used for library synthesis have traditionally been biased toward polar bond formation, such as amide couplings.