Efficient Synthesis of Biologically Active Peptides having Abnormal Amino Acids

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An efficient synthesis of biologically active peptides having abnormal amino acids has been achieved. As a coupling reagent, diphenyl phoshorazidate (DPPA,(C_6H_5O)_2P(O)N_3), diethyl phosphorocyanidate (DEPC,(C_2H_5O)P(O)CN), and pentafluorophenyl diphenylphosphinate (FDPP,(C_6H_5)_2P(O)OC_6F_5) were used. The peptides which we have synthesized are dolastatin 10, microginin, jaspamide, geodiamolide, cyclotheonamide B,alterobactin A,and radiosumin. Parts of theonellamide F and microsclerodermins have been also synthesized. The methods we developed will be suitable for the preparation of these peptides and their analogs on a large scale.