University of Groningen, Department of Drug Design, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands.
Chem Commun (Camb). 2017 Jul 27;53(61):8549-8552. doi: 10.1039/c7cc03370b.
Here we describe the direct usage of C,N-unprotected amino acids in Ugi-tetrazole reactions to produce a novel class of acid-tetrazole compounds. Surprisingly, only the tetrazole Ugi product is found and not traces of other possible Ugi type reactions. Based on this reaction pathway we have designed the synthesis of novel tetrazole-peptidomimetics. A high level of structural diversity can be achieved using this isocyanide based multicomponent reaction (IMCR), providing a platform for the production of functionalized building blocks for novel bioactive molecules and nontraditional scaffolds which previously were not accessible.
在这里，我们描述了 C、N 未保护氨基酸在 Ugi-四唑反应中的直接应用，以产生一类新型的酸-四唑化合物。令人惊讶的是，只发现了四唑 Ugi 产物，而没有其他可能的 Ugi 型反应的痕迹。基于这条反应途径，我们设计了新型四唑肽类似物的合成。使用这种基于异氰化物的多组分反应（IMCR）可以实现高水平的结构多样性，为新型生物活性分子和以前无法获得的非传统支架的功能化构建块的生产提供了一个平台。
