Direct Synthesis of 1_2_Benzisoxazoles Via Palladium Catalysis
钯催化直接合成 1_2_苯并异恶唑
基本信息
- 批准号:9126581
- 负责人:
- 金额:$ 4.87万
- 依托单位:
- 依托单位国家:美国
- 项目类别:
- 财政年份:2014
- 资助国家:美国
- 起止时间:2014-09-04 至 2017-07-07
- 项目状态:已结题
- 来源:
- 关键词:AddressAlzheimer&aposs DiseaseBiologicalCatalysisChemicalsComplexCouplingCyclizationDevelopmentEmploymentEpilepsyFDA approvedFoundationsGoalsHealthIsoxazolesLaboratoriesLeadLeftLigandsMalignant NeoplasmsMedicalMedicineMethodologyMethodsModern MedicineNatureObesityPalladiumPathway interactionsPharmaceutical PreparationsPharmacologic SubstancePhosphinesPreparationProcessReactionRecording of previous eventsRouteSchizophreniaStructureTechnologyWorkantimicrobial drugaryl halidebasecancer typechemical synthesisdesignnitroneobesity treatmentrapid techniquesmall moleculetrendylide
项目摘要
DESCRIPTION (provided by applicant): The 1,2-benzisoxazole heterocycle represents an important chemical motif in modern medicine. Several FDA approved drugs featuring this component, such as Zonisamide and Paliperidone, are widely administered to treat epilepsy and schizophrenia. Other small molecules that contain a 1,2-benzisoxazole are under study for the treatment of Alzheimer's disease, obesity and certain types of cancer. Because these molecules are not found in nature, chemical synthesis is the only route to accessing 1,2-benzisoxazole derivatives. Current methodologies for their laboratory synthesis are chemically and economically inefficient. In order to access new 1,2-benzisoxazole medicines and to optimize derivatives currently under study, a new synthetic method is highly desired. To address this need, a palladium-catalyzed cascade merger of aryl halides and linear nitrones is proposed. This method provides a direct and selective route to 1,2-benzisoxazoles from readily available chemicals. Catalysis allows chemists to prepare complex chemicals under mild reaction conditions; thus, the proposed method will enable the synthesis of 1,2-benzisoxazole derivatives currently inaccessible. This proposal provides strategies inspired by modern technology aided by the rich history of nitrones and palladium catalysis to open new doors for medicinal chemists and ultimately modern medicine.
描述(由申请人提供):1,2-苯并异恶唑杂环代表了现代医学中的重要化学基序。几种FDA批准的含有这种成分的药物,如唑尼沙胺和帕利哌酮,被广泛用于治疗癫痫和精神分裂症。其他含有1,2-苯并异恶唑的小分子正在研究用于治疗阿尔茨海默病,肥胖症和某些类型的癌症。由于这些分子在自然界中没有发现,化学合成是获得1,2-苯并异恶唑衍生物的唯一途径。目前用于其实验室合成的方法在化学和经济上都是低效的。为了获得新的1,2-苯并异恶唑药物并优化目前正在研究的衍生物,非常需要新的合成方法。为了解决这一需求,提出了芳基卤化物和线性硝酮的钯催化级联合并。该方法提供了从容易获得的化学品直接和选择性地制备1,2-苯并异恶唑的途径。催化允许化学家在温和的反应条件下制备复杂的化学品;因此,所提出的方法将使目前无法合成的1,2-苯并异恶唑衍生物成为可能。该提案提供了由硝酮和钯催化的丰富历史辅助的现代技术启发的策略,为药物化学家和最终现代医学打开了新的大门。
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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Jeffrey S Bandar其他文献
Jeffrey S Bandar的其他文献
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{{ truncateString('Jeffrey S Bandar', 18)}}的其他基金
New Synthetic Methodology Enabled by Base-Promoted Halogen and Electron Transfer Processes
碱促进卤素和电子转移过程实现的新合成方法
- 批准号:
10390432 - 财政年份:2020
- 资助金额:
$ 4.87万 - 项目类别:
New Synthetic Methodology Enabled by Base-Promoted Halogen and Electron Transfer Processes
碱促进卤素和电子转移过程实现的新合成方法
- 批准号:
10200852 - 财政年份:2020
- 资助金额:
$ 4.87万 - 项目类别:
New Synthetic Methodology Enabled by Base-Promoted Halogen and Electron Transfer Processes
碱促进卤素和电子转移过程实现的新合成方法
- 批准号:
10028748 - 财政年份:2020
- 资助金额:
$ 4.87万 - 项目类别:
New Synthetic Methodology Enabled by Base-Promoted Halogen and Electron Transfer Processes
碱促进卤素和电子转移过程实现的新合成方法
- 批准号:
10607995 - 财政年份:2020
- 资助金额:
$ 4.87万 - 项目类别:
Direct Synthesis of 1_2_Benzisoxazoles Via Palladium Catalysis
钯催化直接合成 1_2_苯并异恶唑
- 批准号:
8975546 - 财政年份:2014
- 资助金额:
$ 4.87万 - 项目类别: