Solid- and solution-Phase synthesis of highly-Substituted-Pyrrolidine libraries

Starting from a complex bicyclic β-lactam scaffold we have demonstrated the possible production of libraries of a new class of drug-like, highly substituted pyrrolidines. The choice of the type of substitution was made by optimizing various synthetic routes. The selection of each compound is the result of a filtration of a large virtual combinatorial chemical space, using simple criteria. The access to these complex pyrrolidines needed only four to six synthetic steps.