Hubei Province Engineering and Technology Research Center for Fluorinated Pharmaceuticals, School of Pharmaceutical Sciences, Wuhan University, Wuhan 430071, China.
Org Lett. 2021 Apr 2;23(7):2670-2675. doi: 10.1021/acs.orglett.1c00577. Epub 2021 Mar 16.
With PhPCFCOO or TMSCFBr as the difluorocarbene sources, a facile metal-free cycloaddition between heteroconjugated alkenes and difluorocarbene was developed for the highly convergent synthesis of novel difluorinated heterocyclics, including -difluorinated azetidines and 2,3-dihydrobenzofurans. The cycloaddition features high reactivity and regioselectivity, as well as good tolerance of various electron-donating or electron-withdrawing substituents on azaheptafulvenes and -quinone methides.
使用 PhPCFCOO 或 TMSCFBr 作为二氟卡宾源，开发了一种简便的无金属杂共轭烯烃与二氟卡宾的环加成反应，用于高效地合成新型二氟杂环化合物，包括 -二氟氮杂环丁烷和 2,3-二氢苯并呋喃。该环加成反应具有高反应活性和区域选择性，以及对氮杂庚富烯和 -醌甲叉的各种供电子或吸电子取代基的良好耐受性。
