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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(由申请人提供):该提案侧重于新的金属催化加氢酰化和加氢芳基化反应,以形成生物活性分子,如手性胺、差异取代的肼、异吲哚酮和吲唑酮。先前报道的金属催化的加氢酰化方法通常涉及在所有碳-体系的表面上添加酰基和氢化物基团。其中的受体含有杂原子的加氢酰化反应的工作有限。该提案的重点是研究含有多个杂原子(酮亚胺和二氮烯)的系统的金属催化氢酰化和氢芳化反应。这些反应的成功实现后,我们将探索一种C-H活化策略,将生成的手性胺和酰肼分别转化为相应的环状异吲哚酮和吲唑酮。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在药物化学、药物发现和药物研究领域中找到广泛的应用,其允许直接快速组装重要的含氮生物活性分子。
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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