Center for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas 77030, USA.
Org Biomol Chem. 2020 Nov 25;18(45):9221-9226. doi: 10.1039/d0ob02021d.
A zinc bromide-catalyzed synthesis of 5-substituted tetrazoles via DNA-conjugated nitriles using sodium azide has been developed. The protocol offered moderate to excellent yields of tetrazoles with a broad range of substrates, including a variety of functionalized aromatic, heterocyclic, and aliphatic nitriles. In addition, the electronic effect within the substrate scope was evaluated. DNA fidelity was assessed by ligation efficiency and amplifiability analysis. The ability to generate tetrazoles expands the diversity of heterocycles in the preparation of DNA-encoded chemical libraries.
一种通过 DNA 偶联腈利用叠氮化钠实现的锌溴化物催化的 5-取代四唑的合成方法已经开发出来。该方案提供了具有广泛底物范围的中等至优异的四唑产率，包括各种功能化的芳族、杂环和脂肪族腈。此外，还评估了底物范围内的电子效应。通过连接效率和可扩增性分析评估 DNA 保真度。生成四唑的能力扩展了 DNA 编码化学文库制备中杂环的多样性。
