Copper-Catalyzed Alkylation of Silyl Enol Ethers with Sterically Hindered α-Bromocarbonyls: Access to the Histamine H₃ Receptor Antagonist

Dengke Li*

*College of Chemistry and Environmental Science, Qujing Normal University, Qujing, Yunnan 655011, China, Email: dengkeli2011163.com

D. Li, J. Org. Chem., 2021, 86, 609-618.

DOI: 10.1021/acs.joc.0c02277 (free Supporting Information)

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Abstract

A general and efficient copper-catalyzed alkylation of silyl enol ethers with functionalized alkyl bromides provides sterically hindered γ-ketoesters under mild conditions in good yields. The strategy can be used for the synthesis of biologically active histamine H₃ receptor antagonists.

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Key Words

1,4-keto esters

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ID: J42-Y2021