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. 2021 Jan 27;11(8):4842–4852. doi: 10.1039/d0ra07491h

Effect of azide and alkyne orientation and presence of linker on CuAAC cyclization.

Peptide Cyclic peptide Linear peptide precursor % converteda Monomer : dimer
1 (YYTYT-Tz4)cy Fmoc-Pra-YYTYT-Az4 87.4 8.28 : 1
2 (Tz4-YYTYT)cy Fmoc-Az4-YYTYT-Pra 78.8 7.02 : 1
3 (YYTYT-Tz4)cy-(PEG)5 Fmoc-Pra-YYTYT-Az4-(PEG)5 53.5 4.41 : 1
a

Compared to pure linear starting material.