Center for Drug Discovery, Department of Pathology and Immunology, Baylor College of Medicine, Houston, TX, USA.
Methods Mol Biol. 2022;2541:67-73. doi: 10.1007/978-1-0716-2545-3_11.
A key factor for productive DNA-encoded libraries is the chemical diversity of the small molecule moiety attached to an encoding DNA oligomer. The library structure diversity is often limited to DNA-compatible chemical reactions in aqueous media. Herein, we describe a facile process for reducing aryl nitro groups to aryl amines by using sodium dithionite (NaSO). The new protocol offers simple operation and circumvents the pyrophoric potential of the conventional method (Raney nickel). The utility of this method is demonstrated by the versatile synthesis of benzimidazoles on DNA.
对于生产性的 DNA 编码文库来说，一个关键因素是连接到编码 DNA 寡聚物上的小分子部分的化学多样性。文库结构的多样性通常限于水介质中的 DNA 相容化学反应。在此，我们描述了一种通过使用连二亚硫酸钠（NaSO）将芳基硝基还原为芳基胺的简便方法。该新方法操作简单，避免了常规方法（雷尼镍）的易燃性。该方法的实用性通过在 DNA 上的苯并咪唑的多功能合成得到证明。
