Sheng Xia-Xin, Qiu Chao-Ying, Wang Li-Na, Du Yu-Jia, Tang Lu-Ning, Chen Jia-Ming, Liu Guo-Ying, Yang Sen, Zheng Peng-Fei, Chen Ming
Jiangsu Key Laboratory of Advanced Catalytic Materials & Technology, School of Petrochemical Engineering, Changzhou University, 21 Gehu Road, Changzhou, 213164, China.
Department of Clinical and Military Laboratory Medicine, College of Medical Laboratory Science, Army Medical University, No. 30 Gaotanyan Street, Chongqing, 400038, China.
Chemistry. 2024 Nov 12;30(63):e202402402. doi: 10.1002/chem.202402402. Epub 2024 Oct 26.
Efficient transition-metal-free synthesis of benzo[b]azepines and oxindoles is achieved via a radical relay cascade strategy employing halogen atom transfer (XAT) for aryl radical generation followed by intramolecular hydrogen atom transfer (HAT). Optimization yielded moderate to substantial yields under visible light irradiation. Preliminary biological assessments revealed promising anti-tumor activity for select compounds. This study underscores the potential of XAT-mediated radical relay cascades in medicinal chemistry and anticancer drug discovery.
通过自由基接力串联策略，利用卤素原子转移（XAT）生成芳基自由基，随后进行分子内氢原子转移（HAT），实现了苯并[b]氮杂卓和氧化吲哚的高效无过渡金属合成。优化后在可见光照射下可获得中等至较高的产率。初步生物学评估显示，某些化合物具有良好的抗肿瘤活性。这项研究强调了XAT介导的自由基接力串联反应在药物化学和抗癌药物发现中的潜力。
