4.6 Article

Harnessing C-H Activation of Benzhydroxamates as a Macrocyclization Strategy: Synthesis of Structurally Diverse Macrocyclic Isoquinolones

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CHEMISTRY-A EUROPEAN JOURNAL
卷 22, 期 38, 页码 13469-13473

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WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201602332

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C-H activation; isoquinolones; macrocycles; macrocyclization; ruthenium

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  1. Sanofi

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Macrocycles are arising considerable interest in medicinal chemistry. With the goal of harnessing C-H activation reactions for the development of efficient macrocyclization processes, the ruthenium(II)-catalyzed cyclization of O-methyl benzhydroxamates possessing an -acetylenic chain was investigated to access new structurally diverse macrocyclic isoquinolones. A slow addition of the substrate and the presence of Cu(OAc)(2)H2O as an additive were crucial for the success of the macrocyclization that features an excellent functional-group compatibility, as illustrated by the successful synthesis of a library of 21macrocyclic isoquinolones of different ring sizes and substitution patterns. These results contribute to significantly highlight the synthetic interest of C-H activation-mediated processes for the synthesis of new macrocyles incorporating heterocyclic scaffolds of potential interest in medicinal chemistry.

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