非対称ジ(ヘテロアリール)メタンにアクセスするためのパラジウム触媒カスケード二重環化反応
Xing Cai1, Huixuan Zhu1, Xueli Feng1
1Hubei Key Laboratory of Nanomedicine for Neurodegenerative Diseases, School of Chemistry, Chemical Engineering and Life Science, Wuhan University of Technology, Wuhan 430070, China. junniz@whut.edu.cn.
Abstract:
A palladium-catalyzed cascade double annulation reaction for the synthesis of unsymmetrical di(heteroaryl)methanes from non-heteroaryl substrates has been developed. This five-step cascade reaction integrates a furan ring and an indole/isoquinolinone scaffold into a methane molecule through η3-allylpalladium(II)-catalyzed cycloisomerization of β-chlorovinyl ketones followed by allylic heteroarylation, enabling the rapid construction of diverse heteroaryl units with a flexible methylene linker. Furthermore, initial screening indicated that compound 5fa exhibited potential antitumor activity in HeLa cells with the highest inhibition rate among the selected compounds.
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