Jiang Xujuan, Song Yanshan, Peng Junjie, Zhong Zhiying, Chen Li, Zeng Xiaojun
School of Chemistry and Chemical Engineering, Nanchang University, Nanchang, Jiangxi 330031, China.
School of Pharmacy, Nanchang University, Nanchang, Jiangxi 330031, China.
Org Lett. 2023 Nov 17;25(45):8127-8132. doi: 10.1021/acs.orglett.3c03198. Epub 2023 Nov 3.
We report herein a highly efficient copper-catalyzed protocol for the transformation of haloalkynes to the corresponding difluoromethylated alkynes. This scalable protocol exhibits a broad substrate scope and excellent functional group tolerance, enabling the late-stage difluoromethylation of bioactive molecules. Additionally, the strategy of utilizing the difluoromethylalkynes in gram-scale reactions and multiple transformations has proven to be highly valuable in synthetic chemistry.
我们在此报告一种高效的铜催化方法，用于将卤代炔烃转化为相应的二氟甲基化炔烃。这种可扩展的方法具有广泛的底物范围和出色的官能团耐受性，能够实现生物活性分子的后期二氟甲基化。此外，在克级反应和多种转化中利用二氟甲基炔烃的策略已被证明在合成化学中具有很高的价值。
