Studies of Novel and Highly Efficient Peptide Coupling Reagents

doi:10.7523/j.issn.2095-6134.2004.1.020

Abstract

Abstract:

A number of novel and highly efficient immonium-，p yridinium-，thiawlium-，and ben-zimidawlium-type peptide coupling reagents，such asBOMI，BDMP，BPMP，BEP，FEP，BEPH，FEPH，BEMT，and CMB I were designed and synthesized. The high efficiency of these onium salts has been evaluated and proved by model reaction tests and the successful synthesis of various oligopeptides and biologically active peptides both in solution and in the solid phase，for example Leu-enkep halin，the pentapeptide moiety of Dolastatin 15 and the immunosuppressive undecapep-tide Cyclosporin O. Based upon extensive studies of the structure-activity relationship of these coupling reagents，a preliminary guideline for the molecular design of onium-type coupling reagents was developed. These novel reagents have proved to be very useful in the synthesis of structurally challeneine nentides and nentidomimetics.

Key words: coupling reagent, molecular design, peptide synthesis, racemization, reactivity

CLC Number:

O629.72

Li Peng, Xu Jie-cheng. Studies of Novel and Highly Efficient Peptide Coupling Reagents[J]. , 2004, 21(1): 125-134.

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