Palladium‐Catalyzed Suzuki–Miyaura Cross‐Coupling of Heteroaryl‐2‐Boronic Acids with Nitroaryl Halides
Year: 2025
Type: article
Abstract: Heteroaryl‐2‐boronic acids are challenging substrates in the Suzuki–Miyaura cross‐coupling reaction. Here, we report the efficient cross‐coupling of heteroaryl‐2‐boronic acids enabled by using nitro‐substituted aryl halides as the coupling partner under palladium catalysis. The nitro group not only boosts the reactivity of the reaction but also serves as a versatile handle for further functionalization. This method features a broad scope, excellent functional group tolerance, as well as high yields with a low catalyst loading under mild reaction conditions. The utility of the methods is demonstrated by the derivatization of the product and the efficient synthesis of pharmaceutical drug dantrolene.
Authors: Xiaoyuan Zhang, Changhui Wu, Enpeng Wang, Yang Jin, Junhao Xing, Weijun Yao, Xiaowei Dou
Institutions: China Pharmaceutical University, Zhejiang Sci-Tech University
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: hybrid
Estimated APC paid: $4,330
Awards: G7976390852, G8576867690
OpenAlex ID: W4416934934