Nickel-Catalyzed Asymmetric Synthesis of Fully Saturated Nitrogen Heterocycles

 描述（由申请人提供）：完全饱和的氮杂环的对映选择性合成已经受到了大量的关注，这是由于含有该基序的过多的医学相关天然产物和药物。许多已建立的方法集中于碳-氮键的形成，并且固有地限于2-取代杂环的不对称合成。我提出的环化/交叉偶联方法通过构建C2-C3键（一种未充分利用的策略）构建完全饱和的杂环，并允许从外消旋起始材料对映选择性合成取代的氮杂环（3-取代和2，3-二取代的吡咯烷和哌啶）。

 DESCRIPTION (provided by applicant): The enantioselective synthesis of fully saturated nitrogen heterocycles has received a significant amount of attention, owing to the plethora of medicinally relevant natural products and drugs containing this motif. Many of the established approaches focus on formation of the carbon-nitrogen bond and are inherently limited to the asymmetric synthesis of 2-substituted heterocycles. My proposed cyclization/cross-coupling methodology builds fully saturated heterocycles by construction of the C2-C3 bond, an underutilized strategy, and permits the enantioselective synthesis of substituted nitrogen heterocycles (3-substituted and 2,3-disubstituted pyrrolidines and piperidines) from racemic starting materials.