Electrophile-Mediated Enantiospecific Cross-Couplings for the Synthesis of Heterocycles

含氮杂环是一系列生物活性候选药物和天然产物中的重要模体。因此，烷基单元与含氮杂环的SP2-SP3交叉偶联反应是合成的理想目标。然而，目前的方法通常在范围上受到限制，或者表现出较差的选择性。Aggarwal小组致力于通过硼酸酯络合物进行交叉偶联，通过硼酸酯前体与芳基锂试剂反应，然后激活芳环(或杂环)形成。这项工作旨在进一步发展这一化学，用于区域选择性和对映体特异性的SP2-SP3与吡啶和其他含氮芳香族杂环的交叉偶联。

Nitrogen-containing heterocycles are important motifs in a range of bioactive drug candidates and natural products. Hence sp2-sp3 cross coupling reactions of alkyl units to nitrogen-containing heterocycles are a desirable goal in synthesis. However, current approaches are typically limited in scope or display poor selectivity. The Aggarwal group has worked on cross couplings proceeding via boronate complexes, formed by reaction of boronic ester precursors with aryllithium reagents followed by activation of the aromatic ring (or heterocycle). This work seeks to develop this chemistry further for regioselective and enantiospecific sp2-sp3 cross-couplings to pyridines and other aromatic nitrogen-containing heterocycles.