Diamination of Olefins

烯烃的二胺化

• 批准号: 7615745
• 负责人: YIAN SHI
• 金额: $ 27.47万
• 依托单位: COLORADO STATE UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2008
• 资助国家: 美国
• 起止时间: 2008-05-01 至 2012-02-29
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7615745
• 关键词: Address; Alkenes; Area; Development; Diamines; Goals; Indium; Metals; Methods; Nitrogen; Outcome; Pharmacologic Substance; Process; Reaction; Research; Source; System; catalyst

DESCRIPTION (provided by applicant): Vicinal diamines are very important functional moieties which are present in various biologically active compounds and have also been widely used as chiral control elements in asymmetric synthesis. Diamination of olefins presents an attractive strategy for the synthesis of vicinal diamines. While good progress has been made in this area, there are still important problems that remain unsolved. We propose to develop a catalytic diamination process involving diamido metal species to address some of these challenges. The long-term goal of the proposed research is to develop an efficient regio-, diastereo-, and enantioselective catalytic diamination method for olefins with broad scope and the ability to rationalize and predict the stereochemical outcome for a given olefin system. Development of such a method will eventually provide effective synthetic avenues to medicinally important compounds. The specific aims of the proposed research are: (1) to further understand and develop the Pd-catalyzed diamination through studies of reaction mechanism, expansion of substrate scope, and development of a catalytic asymmetric process; (2) to further understand and develop the Cu-catalyzed diamination through studies of reaction mechanism, expansion of substrate scope, and development of a catalytic asymmetric process; (3) to further explore other metal catalysts and nitrogen sources; (4) to explore the synthetic potential of the developed diamination method for the synthesis of useful building blocks and biologically active compounds. PUBLIC HEALTH RELEVANCE: The proposed research is the development of an efficient catalytic diamination method for olefins. The method to be developed will be very useful for the synthesis of medicinal and pharmaceutical compounds.

描述（由申请人提供）：替代二胺是非常重要的功能部分，它们存在于各种生物活性化合物中，并且也已被广泛用作不对称合成中的手性控制元素。烯烃的二胰蛋白酶为综合二胺的合成提供了有吸引力的策略。尽管在这一领域取得了良好的进步，但仍有重要的问题尚未解决。我们建议开发涉及二氨基金属物种的催化胰岛素，以应对其中一些挑战。拟议研究的长期目标是为具有广泛范围的烯烃开发有效的区域，映射和对映选择性催化性催化方法，并具有合理化和预测给定烯烃系统的立体化学结果的能力。这种方法的开发最终将为具有药物重要的化合物提供有效的合成途径。拟议的研究的具体目的是：（1）通过研究反应机制，底物范围的扩展以及催化不对称过程的发展，进一步理解和发展PD催化的胰岛素； （2）通过研究反应机理，底物范围的扩展以及催化不对称过程的发展，进一步理解和发展了Cu催化的胰岛胰岛素； （3）进一步探索其他金属催化剂和氮源； （4）探索开发的胰岛素方法的合成潜力，以合成有用的构建块和生物活性化合物。公共卫生相关性：拟议的研究是开发烯烃的有效催化胰岛素方法。要开发的方法对于合成药用和药物化合物将非常有用。