Efficient Synthesis of Biologically Active Peptides having Abnormal Amino Acids

高效地合成了含有异常氨基酸的生物活性多肽。偶联剂为二苯基磷缩氮酸酯(DPPA，(C6H5O)2P(O)N3)、磷氰酸二乙酯(DEPC，(C2H5O)P(O)CN)和五氟苯基二苯基膦(FDPP，(C6H5)2P(O)OC6F5)。我们所合成的多肽是：多司他丁10、微人参皂苷、茉莉胺、地奥二内酯、环茶酰胺B、另一步甲素和放射性空心素。还合成了茶乙酰胺F和微硬皮病的部分化合物。我们开发的方法将适用于这些多肽及其类似物的大规模制备。

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.