1996 Fiscal Year Final Research Report Summary

Efficient Synthesis of Biologically Active Peptides having Abnormal Amino Acids

Research Project

Project/Area Number	06453190
Research Category	Grant-in-Aid for Scientific Research (B)
Allocation Type	Single-year Grants
Section	一般
Research Field	Chemical pharmacy
Research Institution	NAGOYA CITY UNIVERSITY
Principal Investigator	SHIOIRI Takayuki Nagoya City University, Faculty of Pharmaceutical Sciences, Professor, 薬学部, 教授 (20012627)
Project Period (FY)	1994 – 1996
Keywords	abnormal amino acids / marine peptide / biologically active peptide / sponge / ペプチド縮合試薬
Research Abstract	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.

(3 results)