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

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，使用构型稳定的光学活性亲核剂。通过在最终所需键形成之前建立立体合成中心，可以快速制备用于生物分析的各种单一对映体候选药物文库。光学活性二次亲核试剂的使用将首先在烷基-芳基交叉偶联反应中探索，然后扩展到烷基-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。

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.