Enantioselective Zwitterionic Reactions

对映选择性两性离子反应

基本信息

批准号：
8665818
负责人：
HUW M DAVIES
金额：
$ 35.36万
依托单位：
EMORY UNIVERSITY
依托单位国家：
美国
项目类别：
财政年份：
2011
资助国家：
美国
起止时间：
2011-09-20 至 2015-06-30
项目状态：
已结题

来源：
https://reporter.nih.gov/project-details/8665818
关键词：
Academia Alcohols Alkenes Binding Biological Biological Factors Biomedical Research Chemicals Chemistry Communities Cyclopropanes DNA Sequence Rearrangement Development Drug Industry Drug Targeting Electrons Environment Ethers Goals Indoles Lead Methodology Methods Organic Synthesis Pharmaceutical Preparations Pharmacologic Substance Postdoctoral Fellow Pyrroles Reaction Research Rhodium Scheme Series Source System Training career catalyst coping cycloaddition cyclopropane design drug candidate enol graduate student improved interest novel programs propadiene scaffold ylide

Academia Alcohols Alkenes Binding Biological Biological Factors Biomedical Research Chemicals Chemistry Communities Cyclopropanes DNA Sequence Rearrangement Development Drug Industry Drug Targeting Electrons Environment Ethers Goals Indoles Lead Methodology Methods Organic Synthesis Pharmaceutical Preparations Pharmacologic Substance Postdoctoral Fellow Pyrroles Reaction Research Rhodium Scheme Series Source System Training career catalyst coping cycloaddition cyclopropane design drug candidate enol graduate student improved interest novel programs propadiene scaffold ylide

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项目摘要

DESCRIPTION (provided by applicant): Research Summary The design of new synthetic methods has a broad impact on biomedical research. Many factors are involved in the selection of a compound as a potential drug candidate, but one that is critical, but not always articulated, is whether or not a potential target is accessible. If a compound cannot be made in a practical way either through synthesis or from biological sources, then it will never become a viable pharmaceutical agent. Consequently, truly powerful and previously unprecedented synthetic methods can open up vistas of novel structural scaffolds for exploration as potential drug targets. The central goal of this research program is to develop new strategic reactions that will have broad impact in organic synthesis. Rhodium-stabilized carbenoids containing both donor and acceptor groups are capable of a range of synthetically useful transformations. This proposal focuses on a new direction of study of donor/acceptor carbenoids, namely enantioselective transformations of rhodium-bound zwitterionic intermediates. The full scope of these new synthetic methods will be explored and then applied to the synthesis of biologically relevant natural products and important pharmaceutical drug scaffolds.

描述（由申请人提供）：研究摘要新合成方法的设计对生物医学研究有广泛的影响。选择化合物作为潜在的候选药物的许多因素涉及，但至关重要但并非总是明确的，这是可能的。如果不能通过合成或从生物来源以实用的方式制成化合物，那么它将永远不会成为可行的药物。因此，真正强大且以前前所未有的合成方法可以打开新型结构支架的远景，以作为潜在的药物靶标探索。该研究计划的核心目标是开发新的战略反应，这些反应将对有机综合产生广泛影响。含有供体组和受体组的铑稳定的卡宾类动物具有一系列合成有用的转换。该提议着重于供体/受体卡宾类动物的新方向，即恒河结合的zwitterionic中间体的对映选择性转变。这些新合成方法的全部范围将被探索，然后应用于生物学相关的天然产物和重要的药物支架的合成。