Synthesis of Cyclic Peptides by Alknye-Azide Click Chemistry Cyclization

摘要

@@ Cyclic peptides are widely developed to increase their stability and their bioavailability. Considering the vast number of biologically active cyclic peptides in nature and their potential as drugs in vivo, head-to-tail cyclization of peptide remains an important goal for both academic and industrial laboratories[1,2]. It also poses a significant challenge: not only is oligomerization a possible side reaction, but ring strain in the transition state leading to the cyclic product may prohibit cyclizational together. The use of a 1,4-disubstituted 1,2,3-triazole as an amide bond surrogate and cyclization aid has been reported in recent years. These triazoles have atom placement and electronic properties similar to those of a peptide bond and are accessible in one step via Cu(I) catalyzed alkyne-azide cycloaddition(Figure 1, Scheme 1)[3,4].