Class II Directed Carbometalation Processes for Heterocycle Synthesis

描述(申请人提供)：合成有机化学在发现和生产具有生物和医学意义的分子方面发挥着核心作用。我们实验室的长期目标是推进合成方法和战略，以便在发现此类实体方面找到新的方向。这项建议描述了开发一套合成方法来制备含氮小分子(无环和杂环)。由于这类分子在小分子治疗学的发展中已经相当成功，促进这种结构的构建的方法对于促进生物学、医学和公共健康是重要的。这项工作的中心是发展取代的烯烃和炔烃与氮杂烯丙基环丙烯的双分子碳金属化反应，通过逐步将金属中心与杂二齿有机配体包裹起来实现。综述了烯-1，5-氨基醇、饱和1，5-氨基醇、哌啶类、吡咯类、内酰胺类和吡咯吲哚类化合物的合成新方法。

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.