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Development of New Metal_Catalyzed Hydroacylation and Hydroarylation Processes

Development of New Metal_Catalyzed Hydroacylation and Hydroarylation Processes
新金属催化加氢酰化和加氢芳基化工艺的开发
批准号:
8590847
负责人:
Daniel Tzvi Cohen
金额:
$4.71万
依托单位国家:
美国
项目类别:
财政年份:
2013
资助国家:
美国
项目状态:
已结题
起止时间:
2013-09-01 至 2016-08-31

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项目成果

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中文摘要
翻译
描述(申请人提供):这项建议集中于新的金属催化的氢酰化和氢芳基化反应,以形成生物活性分子,如手性胺、差异取代肼、异吲哚和吲唑酮。以前报道的金属催化的氢酰化反应一般涉及在所有碳链表面加成一个酰基和氢化基。在受体含有杂原子的情况下,氢酰化反应的工作有限。这一建议的重点是研究金属催化的氢酰化和氢芳基化体系,这些体系含有一个以上的杂原子(酮亚胺和双氮烯)。在这些反应成功完成后,我们将探索一种C-H活化策略,将生成的手性胺和肼分别转化为相应的环异吲哚和吲唑酮。除了探索酮亚胺的氢酰化反应外,我们还将研究实现酮亚胺氢芳基化的脱羰基途径。这些方法的成功建立将使重要的含氮生物活性分子能够直接快速组装,从而在药物化学、药物开发和药物研究领域得到广泛应用。
英文摘要
DESCRIPTION (provided by applicant): This proposal focuses on new metal-catalyzed hydroacylation and hydroarylation reactions to form biologically active molecules, such as chiral amines, differentially substituted hydrazines, isoindolones, and indazolones. Previously reported metal-catalyzed hydroacylation processes generally involve the addition of an acyl and hydride group across the face of all carbon ¿-systems. There has been limited work of hydroacylation reactions where the ¿-acceptor contains a heteroatom. The emphasis of this proposal is the investigation of the metal-catalyzed hydroacylation and hydroarylation of ¿-systems that contain one more heteroatoms (ketimines and diazenes). Following the successful achievement of these reactions we will explore a C-H activation strategy to convert the generated chiral amines and hydrazides to the corresponding cyclic isoindolones, and indazolones, respectively. In addition to exploring the hydroacylation of ketimines, we will examine the decarbonylation pathway to achieve the hydroarylation of ketimines. Successful establishment of these methodologies would find wide application in the fields of medicinal chemistry, drug discovery, and pharmaceutical research by allowing for the direct rapid assembly of important nitrogen containing biologically active molecules.
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Development of New Metal_Catalyzed Hydroacylation and Hydroarylation Processes
Development of New Metal_Catalyzed Hydroacylation and Hydroarylation Processes
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