Journal of University of Chinese Academy of Sciences >
Studies of Novel and Highly Efficient Peptide Coupling Reagents
Online published: 2004-01-10
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
Li Peng , Xu Jie-cheng . Studies of Novel and Highly Efficient Peptide Coupling Reagents[J]. Journal of University of Chinese Academy of Sciences, 2004 , 21(1) : 125 -134 . DOI: 10.7523/j.issn.2095-6134.2004.1.020
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