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Bioactive 2‐benzazepines were accessed in an atom‐ and step‐economical manner through a versatile palladium‐catalyzed C−H activation strategy. The C−H arylation required low catalyst loading and a mild base, which was reflected by a broad scope and high functional‐group tolerance. The benzotriazolodiazepinones were identified as new heat shock protein 90 (Hsp90) inhibiting lead compounds, with considerable...
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