Recent progress of on-resin cyclization for the synthesis of clycopeptidomimetics

Abstract Cyclopeptidomimetics are class of cyclopeptides with unnatural linkage. They usually displayed unique constrained structure, enhanced proteolytic stability, and other drug-like character; and have been widely used in medicinal chemistry. Therefore, development of efficient strategies for the synthesis of cyclopeptidomimetics has received many attentions. On-resin cyclization strategy is one of the effective approaches developed to overcome the competing side reaction such as oligomerization and cyclooligomers occurred in solution cyclization. This approach took advantage of the “pseudo-dilution” effect to avoid these undesired by-products and greatly simplified the downstream product purification process. This review summarized the recent on-resin peptide cyclization strategies for the synthesis of cyclopeptidomimetics.

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