Subirós-Funosas Ramon, Nieto-Rodriguez Lidia, Jensen Knud J, Albericio Fernando
Chemistry and Molecular Pharmacology Program, Institute for Research in Biomedicine, Barcelona Science Park, Baldiri Reixac 10, 08028, Barcelona, Spain.
J Pept Sci. 2013 Jul;19(7):408-14. doi: 10.1002/psc.2517. Epub 2013 May 24.
The methodology for peptide bond formation is undergoing a continuous evolution where the main actors are being renewed. In recent years, coupling reagents based on the Oxyma scaffold, such as the uronium salt COMU, has been a groundbreaking contribution to the field. The advantages of COMU over classic benzotriazole-based reagents (HATU, HBTU, HCTU, TBTU) were proven in terms of solubility and coupling efficiency in bulky junctions in our groups and others. However, some aspects of the use of COMU need to be revised and improved, such as the stability of commercial samples in organic solvents, which hampers the compatibility with long synthesis in automated synthesizers. In this review, an overview of the main features and suggestions to improve the use of COMU are presented, along with a discussion on the best conditions for its use in microwave-assisted peptide robots.
肽键形成的方法正在不断发展，其中主要参与者也在不断更新。近年来，基于Oxyma支架的偶联试剂，如脲鎓盐COMU，对该领域做出了开创性贡献。在我们团队和其他团队的研究中，COMU在溶解度和在大分子连接点的偶联效率方面优于经典的基于苯并三唑的试剂（HATU、HBTU、HCTU、TBTU）。然而，COMU的使用在某些方面需要修订和改进，例如商业样品在有机溶剂中的稳定性，这妨碍了其与自动合成仪中长链合成的兼容性。在这篇综述中，将概述COMU的主要特点并提出改进其使用的建议，同时讨论在微波辅助肽机器人中使用COMU的最佳条件。
