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The present invention relates to synthetic methods for 1,2,4-oxadiazole compounds. The general synthetic scheme is:
R1 represents −CH2OtBu or −CH(CH3)OtBu, R3 represents −CH2C(O)NHCPh3, −CH2CH2C(O)NHCPh3, −CH2C(O)OtBu, or −CH2CH2C(O)OtBu, and Aaa is an amino acid residue selected from Thr and Ser; wherein the C-terminus thereof is esterified, and wherein the hydroxy moiety of the side chain of Thr or Ser is substituted with tbutyl; the base is triethylamine; and the solvent is tetrahydrofuran.