Chemistry and Biology Of Multicomponent Reactions

A study was conducted to investigate chemical and biological aspects of multicomponent reactions (MCRs). The high density of atoms of MCR-based compounds played an important role in their propensity for specific target classes where traditional non-MCR compounds had lower screening hit rates. Chemical transformations toward rare scaffold types annotated with unique physicochemical properties were amenable by MCR in a straightforward and short manner. X-ray diffraction investigations revealed that the bicyclic products contain varying degrees of pyramidalization of the bridgehead nitrogen atom. It was also demonstrated that another uniquely shaped scaffold, 3-azabicyclo[4.2.0]octan-4-one derivative was synthesized by combining the Ugi multicomponent reaction with [2 + 2] enone-olefin photochemical transformations.