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首页> 外文期刊>Chemistry: A European journal >Harnessing C-H Activation of Benzhydroxamates as a Macrocyclization Strategy: Synthesis of Structurally Diverse Macrocyclic Isoquinolones
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Harnessing C-H Activation of Benzhydroxamates as a Macrocyclization Strategy: Synthesis of Structurally Diverse Macrocyclic Isoquinolones

机译：利用苯氧肟酸酯的C-H活化作为大环化策略：结构多样的大环异喹啉酮的合成

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摘要

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.
机译：大环化合物在药物化学中引起了极大的兴趣。为了利用C-H活化反应来开发有效的大环化方法，研究了钌（II）催化的具有-炔链的O-甲基苯氧肟酸酯的环化反应，以获取结构上不同的新的大环异喹啉酮。基质的缓慢添加和作为添加剂的Cu（OAc）（2）H2O的存在对于成功实现具有出色的官能团相容性的大环化至关重要，正如成功合成21个大环异喹诺酮文库所说明的那样不同的环尺寸和取代方式。这些结果有助于显着地突出C-H活化介导的方法的合成兴趣，该方法用于合成在药物化学中具有潜在兴趣的杂环支架的新大分子。

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