State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, P. R. China.
School of Pharmaceutical Science and Yunnan Key Laboratory of Pharmacology of Natural Products, Kunming Medical University, Kunming 650500, P. R. China.
Org Lett. 2022 Oct 21;24(41):7533-7537. doi: 10.1021/acs.orglett.2c02824. Epub 2022 Oct 11.
A metal-free regioselective γ-C(sp)-H sulfenylation of enaminones with heterocyclic thiols is reported. This transformation is efficient, mild, scalable, and environmentally friendly and tolerates a large variety of enaminones substrates and heterocyclic thiols. The utility of this strategy is demonstrated in a late-stage modification of bioactive natural products and drug derivatives.
本文报道了一种无金属的区域选择性γ-C(sp3)-H 烯胺酮与杂环硫醇的磺化反应。该转化具有高效、温和、可规模化和环境友好等优点，并且能够容忍各种烯胺酮底物和杂环硫醇。该策略在生物活性天然产物和药物衍生物的后期修饰中得到了应用。
Zotero 插件