Xiao Lin, Liu Xu-Ge, Bao Mei-Zhu, Song Jia-Lin, Chen Shao-Yong, Zheng Yi-Chuan, Liu Yan-Zhi, Zhang Shang-Shi
Center for Drug Research and Development, Guangdong Provincial Key Laboratory of Advanced Drug Delivery, Guangdong Provincial Engineering Center of Topical Precise Drug Delivery System, Guangdong Pharmaceutical University, Guangzhou, 510006, P. R. China.
School of Pharmacy, Henan University, Kaifeng, Henan 475004, China.
Org Lett. 2023 Jul 21;25(28):5185-5190. doi: 10.1021/acs.orglett.3c01614. Epub 2023 Jul 13.
Cp*Rh(III)-catalyzed nitro-directed C-H alkylation/alkenylation of nitroarenes has been reported for the first time. This protocol is associated with the features of high efficiency, broad substrate scope, and good functional group compatibility. Additionally, gram-scale experiments and synthetic applications proved the practicability of the method. Moreover, preliminary mechanistic investigations consistently revealed C-H bond cleavage as the rate-limiting step.
首次报道了Cp*Rh(III)催化的硝基芳烃的硝基导向C-H烷基化/烯基化反应。该方法具有高效、底物范围广、官能团兼容性好等特点。此外,克级实验和合成应用证明了该方法的实用性。此外,初步的机理研究一致表明C-H键裂解是限速步骤。