Li Ke, Qu Yi, An Yulong, Breinlinger Eric, Webster Matthew P, Wen Huanan, Ding Duanchen, Zhao Meng, Shi Xiaodong, Wang Jiangong, Su Wenji, Cui Weiren, Satz Alexander L, Yang Hongfang, Kuai Letian, Little Andrew, Peng Xuanjia
WuXi AppTec (Shanghai) Co., Ltd. 288 Middle Fu Te Road, Shanghai 200131, China.
AbbVie Bioresearch Center, 381 Plantation Street, Worcester, Massachusetts 01605, United States.
Bioconjug Chem. 2020 Sep 16;31(9):2092-2097. doi: 10.1021/acs.bioconjchem.0c00392. Epub 2020 Aug 20.
We report a DNA-compatible protocol for synthesizing amides from DNA-bound aldehydes and non-nucleophilic arylamines including aza-substituted anilines, 2-aminobenzimidazoles, and 3-aminopyrazoles. The reactions were carried out at room temperature and provided reasonable conversions and wide functional group compatibility. The reactions were also successful when employing aryl and aliphatic aldehydes. In addition, qPCR and NGS data suggested no negative impact on DNA integrity after the copper-mediated oxidative amidation reaction.
我们报告了一种与DNA兼容的方法，用于从与DNA结合的醛和非亲核芳基胺（包括氮杂取代的苯胺、2-氨基苯并咪唑和3-氨基吡唑）合成酰胺。反应在室温下进行，具有合理的转化率和广泛的官能团兼容性。使用芳基和脂肪族醛时反应也很成功。此外，定量聚合酶链反应（qPCR）和二代测序（NGS）数据表明，铜介导的氧化酰胺化反应后对DNA完整性没有负面影响。
