Abstract: The present invention relates to new highly functionalized heterobicycle derivatives of general formula (I), prepared by a process which involves only two steps by using, as starting products, commercially available, or easily prepared, &agr;-amino ketones and &agr;,&bgr;-dihydroxy acids or &agr;-amino-&bgr;-hydroxy acids or &agr;-hydroxy-&bgr;-amino acids or &agr;,&bgr;-dithiol acids derivatives and to libraries containing compounds of formula (I) and to the generation of such combinatorial libraries composed of compounds of formula (I), in individual synthesis, mixture synthesis, split and recombine synthesis and parallel synthesis either in manual or automated fashion.