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High Regio‐ and Chemoselectivity [2 + 4] Tandem Annulations Catalyzed by CsF to the Synthesis of 4‐Quinolones under Continuous‐Flow Reactor
Author(s) -
Wang Zhuoyu,
Li Junjie,
Li Weiqiang,
Liu Rong,
Zhang Chunyan,
Gao Sirong,
Liu Teng,
Huang Chao
Publication year - 2025
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.202500016
Subject(s) - chemoselectivity , chemistry , tandem , catalysis , continuous flow , combinatorial chemistry , regioselectivity , organic chemistry , flow chemistry , biochemical engineering , materials science , engineering , composite material
A high regio‐ and chemoselectivity route to the synthesis of 4‐quinolone derivatives involving a CsF‐catalyzed [2 + 4] tandem annulations under continuous‐flow reactor has been developed. This practical and concise protocol between aryne precursors and β ‐enamino diesters provided a range of structurally diverse 4‐quinolones (28 examples) in good to excellent yields. The characteristics of this continuous‐flow are safe operation, high regio‐ and chemoselectivity in a short time. This approach can enrich and develop aryne chemistry, and might provide new opportunities for the discovery of 4‐quinolone drugs.