Palladium/Xu-Phos-Catalyzed Enantioselective Cascade Heck/Intermolecular Direct Heteroarylation Reaction
Kexin Dong , Chao Fang , Zhongyu Li , Bing Xu , Zhan-Ming Zhang , Junliang Zhang
Chinese Journal of Chemistry ›› 2025, Vol. 43 ›› Issue (17) : 2199 -2205.
Palladium/Xu-Phos-Catalyzed Enantioselective Cascade Heck/Intermolecular Direct Heteroarylation Reaction
Asymmetric cascade Heck/C–H functionalization has emerged as an appealing strategy for activating inert C–H bonds and conveniently synthesizing heterocycles with quaternary centers, owing to the domino sequence of carbopalladation followed by C–H functionalization enabling efficient construction of multiple bonds in one pot. Herein, a palladium-catalyzed enantioselective cascade Heck/intermolecular direct heteroarylation reaction of unactivated alkenes with heteroarenes is developed, providing a facile access to diverse bis-heterocycles of great practicality bearing an all-carbon quaternary stereocenter with excellent levels of yields and enantioselectivities under mild conditions. Moreover, the synthetic utility of this strategy is further demonstrated by the versatile transformations of product.
Palladium / Asymmetric catalysis / Quaternary stereocenter / Cascade Heck / C–H functionalization / Heteroarylation
2025 SIOC, CAS, Shanghai, & WILEY-VCH GmbH
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