State Key Laboratory of Natural Medicines, Department of Organic Chemistry, China Pharmaceutical University, No. 24 Tongjiaxiang Road, Nanjing, 210009, P. R. China.
Org Biomol Chem. 2022 Jul 6;20(26):5319-5324. doi: 10.1039/d2ob00834c.
Chlorinated (hetero)anilines are a class of important structural motifs that are widely present in synthetic building blocks and pharmaceuticals. Despite recent advancements, direct aniline chlorination still suffers from / and mono/poly chlorination selectivity problems. Herein, we disclose a photo-redox and organo co-catalyzed chlorination method for anilines. This method has great substrate generality and excellent mono-chlorination selectivity. Another merit of this method is the late-stage modification of drug molecules, which would be useful in medicinal chemistry.
氯化（杂）苯胺是一类重要的结构基序，广泛存在于合成砌块和药物中。尽管最近取得了进展，但直接苯胺氯化仍然存在 / 和单/多氯化选择性问题。在此，我们公开了一种光氧化还原和有机共催化的苯胺氯化方法。该方法具有很大的底物通用性和优异的单氯化选择性。该方法的另一个优点是药物分子的后期修饰，这在药物化学中很有用。
