EnantioBioIso · Enantioselective strategies for the synthesis of phenyl bioisosteres

The obtainment of enantioenriched molecules is of fundamental importance since two enantiomers of the same drug candidate can display completely different biological properties. In recent years, an increasing interest in employing saturated scaffolds has been observed in medicinal chemistry since they provide tridimensionality and well-defined exit vectors that give access to novel unexplored chemical space, leading to a higher success in drug discovery programs. Among them, some polycyclic bridged skeletons have been identified as suitable saturated bioisosteres of aromatic rings which represent the common two-dimensional, flat moieties that are routinely employed in the drug discovery process. The aim of EnantioBioIso is to provide novel enantioselective strategies for the synthesis of phenyl bioisosteres, enabling unprecedented approaches to obtain bridged skeletons that are of fundamental importance for medicinal chemistry.