Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Institute of Antibiotics, School of Pharmacy, Chengdu University, Chengdu 610106, P. R. China.
Org Lett. 2021 Feb 5;23(3):727-733. doi: 10.1021/acs.orglett.0c03950. Epub 2021 Jan 8.
Herein, we report the additive-controlled divergent synthesis of tetrasubstituted 1,3-enynes and alkynylated 3-pyrrolo[1,2-]indol-3-ones through rhodium-catalyzed C-H alkenylation/DG migration and [3+2] annulation, respectively. This protocol features rare directing group migration in 1,3-diyne-involved C-H activation, excellent regio- and stereoselectivity, excellent monofunctionalization over difunctionalization, broad substrate scope, moderate to high yields, good functional group compatibility, and mild redox-neutral conditions.
在这里，我们报告了通过铑催化的 C-H 烯化/DG 迁移和 [3+2] 环加成，分别实现了四取代 1,3-烯炔和炔基化 3-吡咯并[1,2-a]吲哚-3-酮的加控制发散合成。该方案的特点是在涉及 1,3-二炔的 C-H 活化中罕见的导向基团迁移、优异的区域和立体选择性、优异的单官能化胜过双官能化、广泛的底物范围、中等至高产率、良好的官能团兼容性和温和的氧化还原中性条件。
