Ru(II)‐Catalyzed Cascade Regioselective C‐7 and C‐8 Diamidation of Isoquinolinones Using Dioxazolones

ABSTRACT

In this study, we disclose an unprecedented ruthenium‐catalyzed selective C‐7 and C‐8 diamidation of isoquinolinones via weak chelation assistance, employing dioxazolones as an efficient amidating agent. Significantly, in this reaction, dual C─H bonds were functionalized in one pot, enabling isoquinolinones embedded in diamidated scaffolds with high efficiency. The developed protocol enables the efficient synthesis of a broad array of diamidated isoquinolinones derivativities in excellent yields, including pharmaceutically relevant motifs derived from carboxylic acid and fatty acid containing dioxazolones. The resulting products exhibit excellent compatibility toward further synthetic diversification.