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H-bonding promotion of peptide solubility and cyclization by fluorinated alcohols†
Kei Hyugaji,Fayna Garcia-Martin,Shin-Ichiro Nishimura
RSC Advances Pub Date : 02/27/2012 00:00:00 , DOI:10.1039/C2RA01043G
Abstract

A promotion effect for peptide cyclization by strong H-bonding of fluorinated alcohols was revealed via a synthetic study of a cyclic AFGP skeleton. Combination of fluorinated alcohol-DCM solvent system and DIC-additive system afforded the cyclic hexapeptide skeleton in more than 80% yield. The ratio of intra- vs. inter-peptide condensation depended upon the H-bonding donor strength. This effect was quenched by H-bond acceptor solvents.

Graphical abstract: H-bonding promotion of peptide solubility and cyclization by fluorinated alcohols
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