ol1c02546_si_001.pdf (6.04 MB)
RhIII-Catalyzed Direct Heteroarylation of C(sp3)–H and C(sp2)–H Bonds in Heterocycles with N‑Heteroaromatic Boronates
journal contribution
posted on 2021-09-02, 15:04 authored by Huai-Wei Wang, Jia-Xue Wu, Yu-Han Qiao, Yong-Fei Li, Da-Cheng Li, Jian-Min Dou, Qing-Xia Yao, Yi LuHerein,
we disclose a RhIII-catalyzed heteroarylation
of C(sp3)–H and C(sp2)–H bonds
in heterocycles with organoboron reagents. This protocol displays
high efficiency and excellent functional group tolerance. A range
of heterocyclic boronates with strong coordinating atoms, including
pyridine, pyrimidine, pyrazole, thiophene, and furan derivatives,
can be extensively served as the coupling reagents. The direct heteroarylation
method could supply potential application in terms of the synthesis
of drug molecules with multiple heterocycles.
