DOI: 10.1002/adsc.70678 ISSN: 1615-4150

Enantioselective Pd/Cu‐Catalyzed Coupling of α‐Azaaryl‐α‐Fluoroesters With gem ‐Difluorocyclopropanes

Deyue Ren, Jintao Xia, Jinping Hu, Tianhao Li, Jianming Xue, Xiaodan Liu, Guixiang Chen, Fang Xie

We describe an enantioselective fluoroallylation reaction between α‐azaaryl‐α‐fluoroesters and gem ‐difluorocyclopropanes ( gem ‐DFCPs) catalyzed by a Pd/Cu bimetallic system. This transformation provides efficient access to 2‐fluoroallylic esters containing both a tertiary fluorine stereocenter and an azaaryl unit. The protocol tolerates a wide range of substrates and delivers the desired products with good to excellent enantioselectivities under mild reaction conditions. Moreover, the synthetic value of this method is demonstrated through various downstream transformations of the resulting fluoroallylation products.

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