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Strategic Advances in Sequential C-Arylations of Heteroarenes
The Journal of Organic Chemistry ( IF 3.6 ) Pub Date : 2020-12-24 , DOI: 10.1021/acs.joc.0c02151
Savio Cardoza 1 , Manoj Kumar Shrivash 1, 2 , Parthasarathi Das 3 , Vibha Tandon 1
Affiliation  

Sequence-specific C-arylation strategies have important applications in medicinal and material research. These strategies allow C–C bond formations in a regioselective manner to synthesize large molecular libraries for studying structure–activity profiles. The past decade has seen the development of single C–C bond forming reactions using various transition-metal catalysts, cryogenic metalation strategies, and metal-free methods. Sequential arylations of heterocycles allow for the formation of multiaryl derivatives and are a preferred choice over de novo synthetic routes. This perspective sheds light on recent strategic advances to develop various sequential synthetic routes for the multiarylation of heteroarenes. This perspective addresses many challenges in optimizing sequential routes with respect to catalysts, reaction parameters, and various strategies adopted to obtain diversely arylated products.

中文翻译:

杂芳烃顺序C-芳基化的战略进展

序列特异性C-芳基化策略在药物和材料研究中具有重要的应用。这些策略使C–C键的形成具有区域选择性,从而可以合成大分子库来研究结构活性图谱。在过去的十年中,使用各种过渡金属催化剂,低温金属化策略和无金属方法开发了单个C–C键形成反应。杂环的顺序芳基化允许形成多芳基衍生物,并且是从头合成路线的优选选择。该观点为开发杂芳基多元芳构化的各种顺序合成路线的最新战略进展提供了启示。这种观点解决了在优化顺序路线方面的诸多挑战,如催化剂,反应参数,
更新日期:2021-01-16
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