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- W2810402476 endingPage "13157" @default.
- W2810402476 startingPage "13150" @default.
- W2810402476 abstract "Abstract Medium‐ring natural products exhibit diverse biological activities but such scaffolds are underrepresented in probe and drug discovery efforts due to the limitations of classical macrocyclization reactions. We report herein a tandem oxidative dearomatization‐ring‐expanding rearomatization (ODRE) reaction that generates benzannulated medium‐ring lactams directly from simple bicyclic substrates. The reaction accommodates diverse aryl substrates (haloarenes, aryl ethers, aryl amides, heterocycles) and strategic incorporation of a bridgehead alcohol generates a versatile ketone moiety in the products amenable to downstream modifications. Cheminformatic analysis indicates that these medium rings access regions of chemical space that overlap with related natural products and are distinct from synthetic drugs, setting the stage for their use in discovery screening against novel biological targets." @default.
- W2810402476 created "2018-07-10" @default.
- W2810402476 creator A5002081695 @default.
- W2810402476 creator A5004996669 @default.
- W2810402476 creator A5011123032 @default.
- W2810402476 creator A5051167232 @default.
- W2810402476 date "2018-08-02" @default.
- W2810402476 modified "2023-10-09" @default.
- W2810402476 title "Synthesis of Benzannulated Medium-ring Lactams via a Tandem Oxidative Dearomatization-Ring Expansion Reaction" @default.
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