One-Pot Peptide Ligation – Oxidative Cyclization Protocol for the Preparation of Short/Medium Size Disulfide Cyclopeptides

Native chemical ligation (NCL) employing the N-methylbenzimidazolinone (MeNbz) linker readily provided the linear precursor of a 16-mer peptide that is difficult to obtain by stepwise solid-phase peptide synthesis. NCL and the workup conditions were improved toward a protocol that allows for quantitative removal of the 4-hydroxymercapto- phenol additive and subsequent formation of the disulfide bridge in the NCL cocktail by oxidation in air, tolerated by the presence of tris(hydroxypropyl)phosphine.

• Автор: Spengler, Jan (author)
• Інші автори: Blanco Canosa, Juan B. (author), Forni, Luciano (author), Albericio, Fernando (author)
• Формат: article
• Опубліковано: 2018
• Предмети: Ligation–Oxidativ; Cyclopeptides; Disulfide
• Онлайн доступ: https://doi.org/10.1021/acs.orglett.8b01741; http://repositorio.ikiam.edu.ec/jspui/handle/RD_IKIAM/213