Polycomponent Catalysis in Organic Synthesis

有机合成中的多组分催化

• 批准号: 1152996
• 负责人: Thomas Lectka
• 金额: $ 40.5万
• 依托单位: Johns Hopkins University
• 依托单位国家: 美国
• 项目类别: Standard Grant
• 财政年份: 2012
• 资助国家: 美国
• 起止时间: 2012-09-01 至 2015-08-31
• 项目状态: 已结题
• 来源: https://www.nsf.gov/awardsearch/showAward?AWD_ID=1152996&HistoricalAwards=false
• 关键词: Polycomponent; Catalysis; Organic; Synthesis

In this project funded by the Chemical Synthesis (SYN) Program, Prof. Thomas Lectka of Johns Hopkins University develops new chemical methods that employ several independent catalysts working synergistically to produce chemically interesting and useful products not easily accessible in other ways. Besides theoretical interest, operational simplicity, low catalyst loadings, mutual compatibility, and broad scope will be fundamental goals as well. The foundation of the approach will be polycomponent catalysis (for example, a catalytic nucleophile in combination with an organometallic complex, a Lewis acid, and/or a phase transfer catalyst) that results in powerful methods for the synthesis of pharmaceutically relevant functionalized targets, including chiral fluorides, alkaloids, lactams and related compounds. A focus on new methods of fluorination is especially noted; fluorinated organic molecules provide fruitful and exciting new leads for drug discovery.This project would serve three main goals: 1) the development of complex yet highly worthwhile new chemical processes; 2) fundamentally new approaches to the synthesis of pharmaceutically relevant targets and other useful molecules; 3) and practical training in synthetic chemistry for graduate students (including members of underrepresented groups). Equally, exposure of numerous undergraduates to synthetic projects (especially at hospital-oriented Johns Hopkins) will help to prepare them for careers in health-related occupations.

在这个由化学合成 (SYN) 计划资助的项目中，约翰·霍普金斯大学的 Thomas Lectka 教授开发了新的化学方法，该方法采用几种独立的催化剂协同工作，以生产其他方式不易获得的化学有趣且有用的产品。 除了理论兴趣之外，操作简单性、低催化剂负载、相互兼容性和广泛的范围也将是基本目标。 该方法的基础是多组分催化（例如，催化亲核试剂与有机金属配合物、路易斯酸和/或相转移催化剂的组合），从而产生用于合成药物相关功能化靶标的强大方法，包括手性氟化物、生物碱、内酰胺和相关化合物。 特别值得注意的是对新氟化方法的关注；氟化有机分子为药物发现提供了富有成效且令人兴奋的新线索。该项目将实现三个主要目标：1）开发复杂但非常有价值的新化学工艺； 2）合成药学相关靶点和其他有用分子的全新方法； 3）以及为研究生（包括代表性不足群体的成员）提供合成化学实践培训。 同样，让众多本科生接触综合项目（特别是在以医院为导向的约翰霍普金斯大学）将有助于他们为健康相关职业的职业生涯做好准备。