Class II Directed Carbometalation Processes for Heterocycle Synthesis

用于杂环合成的 II 类定向碳金属化工艺

• 批准号: 8037034
• 负责人: GLENN C MICALIZIO
• 金额: $ 36.87万
• 依托单位: SCRIPPS FLORIDA
• 依托单位国家: 美国
• 财政年份: 2007
• 资助国家: 美国
• 起止时间: 2007-03-12 至 2012-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8037034
• 关键词: Alkenes; Alkynes; Amino Alcohols; Architecture; Biological; Biological Factors; Biology; Carbon Dioxide; Complex; Coupling; Development; Goals; Laboratories; Lactams; Ligands; Mediating; Medical; Medicine; Metals; Methods; Molecular; Nitrogen; Organic Chemistry; Pathway interactions; Pattern; Pharmacologic Substance; Play; Preparation; Principal Investigator; Process; Production; Public Health; Pyrroles; Reaction; Research; Research Activity; Research Proposals; Role; Site; System; Therapeutic; Work; base; dihydroxythiobinupharidine; ditryptophenaline; method development; novel therapeutics; piperidine; programs; small molecule

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.

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策略，为发现此类实体提供新的方向。该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治疗剂的开发中已经相当成功，因此促进这种结构的构建的方法对于推进生物学、医学和公共卫生是重要的。这项工作的中心焦点是取代的烯烃和炔与氮杂金属环丙烯的双分子碳化反应的发展，使逐步封装的金属中心与杂二齿有机配体。总之，我们描述了合成烯-1，5-氨基醇，饱和1，5-氨基醇，哌啶，吡咯，内酰胺和吡咯并吲哚啉的新方法。