In this study, we developed an efficient approach for the synthesis of 2-amino-1,3,4-oxadiazoles that are bioisosteres of the amide functional group. The synthesized oxadiazoles were conjugated to octa- and nonapeptides through the C- or N-terminus as precursors of leuprolide acetate. The synthesized compounds are peptidomimetics of leuprolide acetate.