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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的氢酰化和氢芳基化反应,以形成具有生物活性的分子,如手性胺,差异取代肼,异吲哚酮和吲唑酮。先前报道的金属催化的氢酰化过程通常涉及在所有碳体系的表面加成酰基和氢化物基团。对于含有杂原子的受体的氢酰化反应,已有有限的研究。本提案的重点是研究含有多一个杂原子(酮胺和二氮)的金属催化的氢化酰基化和氢化芳基化。在这些反应成功实现之后,我们将探索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酮和吲达唑酮。除了探索酮胺的氢酰化,我们将研究脱羰基化途径来实现酮胺的氢芳基化。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得到广泛应用,因为它允许直接快速组装含有生物活性分子的重要氮。
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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