Ligand-Promoted Enantioselective C-H Activation Reaction
配体促进的对映选择性 C-H 活化反应
基本信息
- 批准号:10439915
- 负责人:
- 金额:$ 58.58万
- 依托单位:
- 依托单位国家:美国
- 项目类别:
- 财政年份:2008
- 资助国家:美国
- 起止时间:2008-08-01 至 2025-06-30
- 项目状态:未结题
- 来源:
- 关键词:AcetatesAcidsAcute respiratory failureAddressAldehydesAmidesAminesAttenuatedBindingCarbonCarboxylic AcidsChelating AgentsCollaborationsCouplingCysteineDevelopmentDistalDrug IndustryHydrogen BondingKetonesLaboratoriesLactamsLactonesLigand BindingLigandsMediatingMetalsMethodsOrganic SynthesisOxidantsPharmaceutical PreparationsPreparationProteinsPyridonesReactionResearchSerine HydrolaseSilverSourceTechnologyactivity-based protein profilingcarbenecatalystchelationcovalent bonddesigndrug candidatedrug discoveryhuman diseaseinhibitorneutrophil elastase inhibitornovelnovel strategiesnovel therapeuticsprogramsquinolinerecruitscaffoldsuccesstert-Butylhydroperoxidethioether
项目摘要
Project Summary
Desymmetrizing activation of prochiral C–H bonds via metal insertion has emerged as a potentially
transformative approach for the rapid and divergent synthesis of chiral compounds. However, a significant
challenge prohibiting the broad utility of this approach is the poor reactivity of native substrates in the absence
of externally-appended directing groups. This proposal directly addresses this challenge by developing two
approaches to achieve the enantioselective C–H activation of a range of native substrates commonly found in
organic synthesis and drug discovery—carboxylic acids, ketones, aldehydes and amines: (A) Development of
chiral bidentate L,X-type ligands containing N-acetyl or pyridone motifs to accelerate C–H cleavage; (B)
Development of chiral transient directing groups (TDGs) to enable enantioselective C–H activation of ketones,
aldehydes and amines. Following initial discoveries of chiral ligands and TDGs, we will then develop various
catalytic cycles to enable the enantioselective C–H activation of diverse native substrates, forming a range of
carbon–carbon and carbon–heteroatom bonds asymmetrically. These novel reactions will provide a versatile
platform for the construction of -, -, and -stereocenters. These technologies will be applied to drug
discovery in collaboration with the pharmaceutical industry and academic laboratories. Specifically, the one-
step access to the atypical chiral -lactones and lactams via enantioselective C–H activation will be applied to
the discovery of covalent inhibitors for serine hydrolases and cysteine-dependent proteins using activity-based
protein profiling.
项目总结
项目成果
期刊论文数量(0)
专著数量(0)
科研奖励数量(0)
会议论文数量(0)
专利数量(0)
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Jin-Quan Yu其他文献
Jin-Quan Yu的其他文献
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{{ truncateString('Jin-Quan Yu', 18)}}的其他基金
Catalyst-Controlled Site-Selective C-H Functionalizations of Arenes and Heteroarenes
芳烃和杂芳烃的催化剂控制位点选择性 C-H 官能化
- 批准号:
10461954 - 财政年份:2012
- 资助金额:
$ 58.58万 - 项目类别:
Catalyst-Controlled Site-Selective C-H Functionalizations of Arenes and Heteroarenes
芳烃和杂芳烃的催化剂控制位点选择性 C-H 官能化
- 批准号:
10657626 - 财政年份:2012
- 资助金额:
$ 58.58万 - 项目类别:
Catalyst-Controlled, Site-Selective C-H Functionalization of Heterocycles
杂环化合物的催化剂控制、位点选择性 C-H 官能化
- 批准号:
8539807 - 财政年份:2012
- 资助金额:
$ 58.58万 - 项目类别:
Catalyst-Controlled, Site-Selective C-H Functionalization of Heterocycles
杂环化合物的催化剂控制、位点选择性 C-H 官能化
- 批准号:
8341688 - 财政年份:2012
- 资助金额:
$ 58.58万 - 项目类别:
Catalyst-Controlled Site-Selective C-H Functionalizations of Arenes and Heteroarenes
芳烃和杂芳烃的催化剂控制位点选择性 C-H 官能化
- 批准号:
10254416 - 财政年份:2012
- 资助金额:
$ 58.58万 - 项目类别:
Catalyst-Controlled, Site-Selective C-H Functionalization of Heterocycles
杂环化合物的催化剂控制、位点选择性 C-H 官能化
- 批准号:
8704957 - 财政年份:2012
- 资助金额:
$ 58.58万 - 项目类别:
Ligand-Promoted Enantioselective C-H Activation Reaction
配体促进的对映选择性 C-H 活化反应
- 批准号:
10651648 - 财政年份:2008
- 资助金额:
$ 58.58万 - 项目类别:
Development of carboxyl- and amide-directed C-H activation/C-C coupling reactions
羧基和酰胺定向的 C-H 活化/C-C 偶联反应的开发
- 批准号:
8073652 - 财政年份:2008
- 资助金额:
$ 58.58万 - 项目类别:
Ligand-Promoted Enantioselective C-H Activation Reaction
配体促进的对映选择性 C-H 活化反应
- 批准号:
10299074 - 财政年份:2008
- 资助金额:
$ 58.58万 - 项目类别:
Ligand-promoted Enantioselective and Remote C-H Activation Reactions
配体促进的对映选择性和远程 C-H 激活反应
- 批准号:
8691885 - 财政年份:2008
- 资助金额:
$ 58.58万 - 项目类别:
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