Stereospecific Nickel-Catalyzed Cross-Coupling for Pharmacophore Synthesis

用于药效团合成的立体特异性镍催化交叉偶联

• 批准号: 8373617
• 负责人: Elizabeth Reinhardt Jarvo
• 金额: $ 27.3万
• 依托单位: UNIVERSITY OF CALIFORNIA-IRVINE
• 依托单位国家: 美国
• 财政年份: 2012
• 资助国家: 美国
• 起止时间: 2012-09-01 至 2017-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/8373617
• 关键词: Address; Alcohols; Antineoplastic Agents; Biological; Biological Factors; Biomedical Research; Carbon; Chemicals; Clinical Trials; Complement; Complex; Coupling; Development; Electrons; Ethers; Goals; Knowledge; Lead; Marketing; Methods; Nickel; Organic Synthesis; Organometallic Chemistry; PC3 cell line; Pharmaceutical Chemistry; Pharmacologic Substance; Positioning Attribute; Preparation; Production; Reaction; Reagent; Research; Synthesis Chemistry; Testing; Therapeutic; Transition Elements; Translating; Tubulin; Work; analog; base; catalyst; chemical reaction; design; pharmacophore; polymerization; research study; stereochemistry

DESCRIPTION (provided by applicant): This proposal outlines the development of new chemical methods for alkyl-alkyl cross- coupling reactions to form carbon-carbon bonds. The objectives of this project are to generate new strategies for stereospecific cross-coupling reactions, where the stereochemical information from the electrophilic reaction partner is translated to the newly formed stereogenic center of the product. These methods will be utilized in the synthesis of di- and triarylmethane analogs of anticancer agents. The development of these reactions will directly impact the development of new pharmaceutical agents by providing new methods for their preparation. PUBLIC HEALTH RELEVANCE: The development of new chemical methods for organic synthesis is essential in the preparation of natural products and other bioactive molecules for preliminary biological studies, clinical trials, and production for market. Despite the advanced state of synthetic chemistry serious challenges remain. This proposal describes the development of new chemical reactions that will address one of these challenges, cross-coupling reactions that form tertiary stereogenic centers with control of absolute stereochemistry.

描述（由申请人提供）：本提案概述了烷基-烷基交叉偶联反应形成碳-碳键的新化学方法的发展。本项目的目标是产生立体特异性交叉偶联反应的新策略，其中来自亲电反应伙伴的立体化学信息被转化为新形成的产物的立体中心。这些方法将用于二芳基甲烷和三芳基甲烷类似物的合成。这些反应的发展将为新药的制备提供新的方法，从而直接影响新药的开发。