Solid- and solution-phase synthesis of highly-substituted-pyrrolidine libraries

Starting from a complex bicyclic beta -lactam scaffold we have demonstrated the possible production of libraries of a new class of drug-like, highly s ubstituted 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, us ing simple criteria. The access to these complex pyrrolidines needed only f our to six synthetic steps. (C) 2001 Elsevier Science Ltd. All rights reser ved.