广州医科大学阮志雄团队报道了和或在水中电偶合成远端氨基醇。相关研究成果发表在近日出版的《德国应用化学》。

氨基醇，特别是远端氨基醇和肽醇，由于其在生物活性化合物中的功能多样性而具有价值。然而，传统的合成方法面临着重大挑战，使电化学成为一种有吸引力的替代方法。

该文中，研究人员开发了一种温和且生物相容的顺序配对电解策略，利用铜电催化合成各种远程氨基醇，包括非天然肽醇。

实验结果和密度泛函理论（DFT）计算均表明，水既是羟基来源又是溶剂，有助于在阴极与Cu（I）生成CuH，从而减少反应过程中形成的醛中间体。

附：英文原文

Title: Paired Electro-Synthesis of Remote Amino Alcohols with/in H2O

Author: Zhixiong Ruan, Xinyue Fang, Xinwei Hu, Quan-Xin Li, Shao-Fei Ni

Issue&Volume: 32024-11-13

Abstract: Amino alcohols, particularly remote amino alcohols and peptide alcohols, are valuable due to their functional diversity in biologically active compounds. However, traditional synthesis methods face significant challenges, making electrochemistry an attractive alternative. We have developed a mild and biocompatible sequential paired electrolysis strategy, leveraging copper-electrocatalysis to synthesize diverse remote amino alcohols, including unnatural peptide alcohols. Both experimental results and density functional theory (DFT) calculations demonstrate that water serves as both the hydroxyl source and the solvent, facilitating the generation of CuH with Cu(I) at the cathode, which in turn reduces the aldehyde intermediates formed during the reaction.

DOI: 10.1002/anie.202418277

Source: https://onlinelibrary.wiley.com/doi/10.1002/anie.202418277