Class II Directed Carbometalation Processes for Heterocycle Synthesis

描述（由申请人提供）：合成有机化学在发现和生产具有生物学和医学意义的分子方面起着核心作用。我们实验室的长期目标是推进合成方法和策略，为发现这些实体提供新的方向。本提案描述了一套用于制备含氮小分子（无环和杂环）的合成方法的发展。由于这类分子在小分子疗法的发展中取得了相当大的成功，因此促进此类结构构建的方法对于推进生物学、医学和公共卫生都很重要。本工作的中心重点是发展取代烯烃和炔烃与叠氮金属环丙烯的双分子碳金属化反应，通过用异齿有机配体逐步包封金属中心来实现。总的来说，我们描述了合成烯-1,5-氨基醇、饱和1,5-氨基醇、哌啶、吡咯、内酰胺和吡咯啉的新方法。

DESCRIPTION (provided by applicant): Synthetic organic chemistry plays a central role in the discovery and production of molecules with biological and medical significance. The long-term goal of our laboratory is to advance synthetic methods and strategies that allow for new directions in the discovery of such entities. This proposal describes the development of a suite of synthetic methods for the preparation of nitrogen-containing small molecules (acyclic and heterocyclic). As molecules of this class have been quite successful in the development of small molecule therapeutics, methods that facilitate the construction of such architectures are important for advancing biology, medicine, and public health. The central focus of this work is the development of bimolecular carbometalation reactions of substituted olefins and alkynes with azametallacyclopropenes, enabled by stepwise encapsulation of the metal center with heterobidentate organic ligands. Overall, we describe new methods for the synthesis of ene-1,5-aminoalcohols, saturated 1,5-aminoalcohols, piperidines, pyrroles, lactams and pyrroloindolines.