Meta and para-C-H Functionalization of Pyridines and Pyridine Editing
Meta and para-C-H Functionalization of Pyridines and Pyridine Editing
批准号:
523187418
负责人:
Professor Dr. Armido Studer
金额:
$0.0万
依托单位国家:
德国
项目类别:
Research Grants
财政年份:
--
资助国家:
德国
项目状态:
未结题
起止时间:
中文摘要
吡啶类、喹啉类和异喹啉类化合物区域选择性元功能化的新合成方法将得到发展。所应用的策略使用去芳构化-再芳构化方法,其中实际的碳氢功能化是通过去芳构化的二胺中间体发生的。所开发的方法应非常稳健,并适用于更大规模,以证明其与农化和制药工业的相关性。自由基和亲电的碳氢官能化将被探讨。沿着这些路线,药理学上有趣的功能将使用开发的方法在吡啶位上介绍。此外,将探索自由基/离子序列吡啶c - h功能化的合成方法,以合成具有完全区域控制的元、元、准三功能化吡啶。最后,将讨论吡啶编辑。
英文摘要
Novel synthetic methodology for the regioselective meta-functionalization of pyridines, quinolines, and isoquinolines will be developed. The strategy applied uses a dearomatization-rearomatization approach, where the actual C-H-functionalization occurs through dearomatized dienamine intermediates. The methods developed should be very robust and applicable on larger scale to document their relevance for agrochemical and pharmaceutical industry. Radical as well as electrophilic C-H-functionalizations will be explored. Along these lines, pharmacologically interesting functionalities will be introduced at the pyridine meta-position using the developed methods. Further, synthetic methodology for the radical/ionic sequential pyridine C-H-functionalization that allows the synthesis of meta, meta’, para-trifunctionalized pyridines with complete regiocontrol will be explored. Finally, pyridine editing will be addressed.
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