Catalytic Methods for Rapid Aromatic Derivatization
Catalytic Methods for Rapid Aromatic Derivatization
批准号:
9154613
负责人:
David A Nicewicz
金额:
$27.68万
依托单位国家:
美国
项目类别:
财政年份:
2016
资助国家:
美国
项目状态:
已结题
起止时间:
2016-09-20 至 2020-07-31
关键词:
AirAlcoholsAromatic CompoundsBoronic AcidsCatalysisChemicalsComplexCouplingDental crownsDevelopmentDyesEvaluationFluoridesGoalsLeadLibrariesMetabolicMethodsMolecularNitrogenOxidantsOxygenPharmaceutical ChemistryPharmacologic SubstancePlayProtocols documentationReactionReagentReportingResearchResearch PersonnelResearch ProposalsRoleSourceStructureSystemTherapeuticTransition ElementsVisible Radiationaryl halidebasecatalystchemical reactiondesigndrug candidateflexibilityfunctional grouphalogenationlipophilicitynovelnovel strategiesprogramsrapid techniquescaffoldsmall molecule librariessmall molecule therapeuticstool
中文摘要
项目摘要
本研究提案的目标是开发直接C-H的新催化方案
芳香族化合物的官能化。芳香族化合物是大自然中的中心图案,
大多数治疗方法和简单的方法,他们的进一步阐述总是在需求。
该研究计划的目标是为生物医学研究人员生成新的合成工具
为了能够衍生化含先导芳香族的治疗剂,
候选药物进行进一步评估。该提案描述了有机染料的用途,
催化剂来实现十几种新的化学转化。建议的价值
合成方法的一个优点是利用未预氧化的芳族化合物的能力,从而允许更大的合成。
可以采用的芳族结构类型的灵活性。我们预测这项研究
计划将提高药物化学家的合成能力,探索更大的
化学空间在小分子疗法的发展。
英文摘要
Project Summary
The objective of this research proposal is to develop new catalytic protocols for the direct C–H
functionalization of aromatic compounds. Aromatic compounds are central motifs in the vast
majority of therapeutics and simple methods for their further elaboration are always in demand.
The goal of this research program is to generate new synthetic tools for biomedical researchers
to be able to derivatize lead aromatic-containing therapeutics in order to assemble libraries of
drug candidates for further evaluation. This proposal describes the use of organic dyes as
catalysts to enable over a dozen new chemical transformations. The value of the proposed
synthetic methods is the ability to utilize aromatics that are not pre-oxidized, allowing for greater
flexibility in the types of aromatic structures that can be employed. We predict that this research
program will enhance the synthetic capabilities of medicinal chemists to explore greater
chemical space in the development of small molecule therapeutics.
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会议论文
New Catalytic Methods for the Synthesis of Complex Molecules
-
批准号:10597994
-
项目类别:
-
资助金额:$55.89万
-
财政年份:2020
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负责人:David A Nicewicz
-
依托单位:
New Catalytic Methods for the Synthesis of Complex Molecules
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批准号:10395487
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项目类别:
-
资助金额:$55.89万
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财政年份:2020
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负责人:David A Nicewicz
-
依托单位:
Catalytic Methods for Rapid Aromatic Derivatization
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批准号:9750737
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项目类别:
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资助金额:$27.68万
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财政年份:2016
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负责人:David A Nicewicz
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依托单位:
Catalytic Enantioselective Cation Radical-Mediated Transformations
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批准号:8540442
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项目类别:
-
资助金额:$28.56万
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财政年份:2011
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负责人:David A Nicewicz
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依托单位:
Catalytic Enantioselective Cation Radical-Mediated Transformations
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批准号:8324505
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项目类别:
-
资助金额:$29.59万
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财政年份:2011
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负责人:David A Nicewicz
-
依托单位:
Catalytic Enantioselective Cation Radical-Mediated Transformations
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批准号:8728946
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项目类别:
-
资助金额:$29.59万
-
财政年份:2011
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负责人:David A Nicewicz
-
依托单位:
Catalytic Enantioselective Cation Radical-Mediated Transformations
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批准号:8158605
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项目类别:
-
资助金额:$29.59万
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财政年份:2011
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负责人:David A Nicewicz
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依托单位:
Organocatalytic Asymmetric Cascade Reactions
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批准号:7425314
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项目类别:
-
资助金额:$4.68万
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财政年份:2007
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负责人:David A Nicewicz
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依托单位:
Organocatalytic Asymmetric Cascade Reactions
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批准号:7758098
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项目类别:
-
资助金额:$2.46万
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财政年份:2007
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负责人:David A Nicewicz
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依托单位:
Organocatalytic Asymmetric Cascade Reactions
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批准号:7052299
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项目类别:
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资助金额:$4.4万
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财政年份:2007
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负责人:David A Nicewicz
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依托单位:
海外基金