Carbon Dioxide Activation Center (CADIAC), Department of Chemistry and the Interdisciplinary Nanoscience Center (iNANO), Aarhus University, Gustav Wieds Vej 14, 8000, Aarhus C, Denmark.
Department of Medicinal Chemistry, Uppsala University, 75123, Uppsala, Sweden.
Angew Chem Int Ed Engl. 2017 Apr 10;56(16):4549-4553. doi: 10.1002/anie.201700446. Epub 2017 Mar 16.
A mild and effective method is described for C-labeling of peptides selectively at the N-terminal nitrogen or at internal lysine positions. The presented method relies on the use of specific biphosphine palladium-methyl complexes and their high reactivity towards amino-carbonylation of amine groups in the presence [ C]carbon monoxide. The protocol facilitates the production of native N- C-acetylated peptides, without any structural modifications and has been applied to a selection of bioactive peptides.
本文描述了一种温和有效的方法，可选择性地在 N 末端氮原子或内部赖氨酸位置对肽进行 C 标记。该方法依赖于使用特定的双膦钯-甲基配合物及其在 [ C]一氧化碳存在下对胺基羰基化反应的高反应性。该方案有利于生产天然的 N- C-乙酰化肽，而不会造成任何结构修饰，并已应用于一系列生物活性肽。
