Metal-Catalyzed Cross-Coupling Reactions Using Optically-Active Nucleophiles

使用光学活性亲核试剂的金属催化交叉偶联反应

• 批准号: 8286884
• 负责人: Mark Roger Biscoe
• 金额: $ 14.68万
• 依托单位: CITY COLLEGE OF NEW YORK
• 依托单位国家: 美国
• 财政年份: 2011
• 资助国家: 美国
• 起止时间: 2011-07-01 至 2014-04-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8286884
• 关键词: Architecture; Biological; Biological Assay; Carbon; Coupling; Data; Development; Goals; Hydrogenation; In Situ; Individual; Kinetics; Libraries; Ligands; Metals; Methods; Molecular; Optics; Organotin Compounds; Pharmacologic Substance; Preparation; Process; Reaction; Reagent; Research; Research Personnel; Route; Techniques; Testing; Transition Elements; Vinyl Compounds; Work; aryl halide; computer studies; drug candidate; drug discovery; enantiomer; interest; programs

DESCRIPTION (provided by applicant): We aim to develop new, general methods for obtaining non-racemic biologically-active molecules using transition metal-catalyzed carbon-carbon bond-forming reactions that employ configurationally-stable, optically-active nucleophiles. By establishing the stereogenic center prior to the formation of the final desired bond, the rapid preparation of diverse libraries of single-enantiomer drug candidates for use in biologic assays will be achievable. The use of optically-active secondary nucleophiles will be initially explored in alkyl-aryl cross-coupling reactions and extended to alkyl-alkyl cross-coupling reactions in order to maximize access to chiral structural motifs that are currently inaccessible but are of biological or pharmaceutical interest.

描述（由申请人提供）：我们的目标是开发新的，通用的方法来获得非外消旋生物活性分子，使用过渡金属催化的碳-碳键形成反应，采用构型稳定，光学活性的亲核试剂。通过在最终所需键形成之前建立立体中心，可以快速制备用于生物分析的各种单对映体候选药物文库。光学活性二级亲核试剂的使用将首先在烷基-芳基交叉偶联反应中进行探索，并扩展到烷基-烷基交叉偶联反应，以便最大限度地获得目前无法获得但具有生物学或药学意义的手性结构基序。