Synthesis method of cyclopeptide containing maleimide acid

Abstract

The invention relates to the field of polypeptide synthesis, in particular to a synthesis method of cyclopeptide containing maleimide acid. The method comprises the following steps: carrying out solid-phase synthesis by using resin to obtain side chain full-protection peptide-resin containing maleimide acid, cracking by using a hexafluoroisopropanol solution to obtain full-protection peptide, carrying out cyclization reaction in the presence of condensation reagents EDCI and OXYMA to obtain full-protection cyclic peptide, and removing a protecting group to obtain the cyclic peptide. According to the cyclic peptide synthesis method disclosed by the invention, in the steps of full-protection cracking and cyclization, the cyclic peptide does not need to be adjusted to be alkaline, a maleimide ring structure cannot be damaged, and side reactions are reduced; a hexafluoroisopropanol solution is used as a full-protection cracking reagent, p-methoxytrityl or p-methyltrityl protecting groups on amino groups are removed while the full-protection peptide is cracked from the resin, and the full-protection peptide is obtained; eDCI and OXYMA are used as cyclization condensation reagents, and the cyclization effect is good. According to the cyclic peptide synthesis method disclosed by the invention, a cyclic peptide product with relatively high purity can be obtained.

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