Application and Development of New Radical Synthetic Methods

自由基合成新方法的应用与发展

• 批准号: RGPIN-2015-05856
• 负责人: Sammis, Glenn
• 金额: $ 2.55万
• 依托单位: University of British Columbia
• 依托单位国家: 加拿大
• 项目类别: Discovery Grants Program - Individual
• 财政年份: 2015
• 资助国家: 加拿大
• 起止时间: 2015-01-01 至 2016-12-31
• 项目状态: 已结题
• 来源: https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=590681
• 关键词: Application; Development; New; Radical; Synthetic

This proposal focuses on the development of new technologies for the synthesis of molecules that are of interest to the pharmaceutical and agrochemical industries. A key goal is the development of new methods for fluorine incorporation into medicinal agents. While not common in natural organisms, fluorine is a valuable component of many bioactive molecules. Currently, over 20% of the top selling pharmaceutical agents contain fluorine. While fluorine is medicinally useful, it is often difficult to incorporate into molecules. The first and second portions of this proposal focus on new technologies for the synthesis of particularly challenging fluorinated motifs using organic free radicals. We will access the key radical intermediates using several different methods, including UV light. We will also investigate new technology using more environmentally-friendly and lower-energy visible light in combination with photoredox catalysis.

这项提议的重点是开发新的技术，用于合成制药和农化工业感兴趣的分子。一个关键的目标是开发将氟结合到药物中的新方法。虽然氟在天然生物体中并不常见，但它是许多生物活性分子的宝贵成分。目前，最畅销的药剂中有20%以上含有氟。虽然氟在医学上是有用的，但它通常很难被结合到分子中。该提案的第一部分和第二部分侧重于使用有机自由基合成特别具有挑战性的氟化基序的新技术。我们将使用几种不同的方法来获取关键的自由基中间体，包括紫外光。我们还将研究使用更环保和更低能量的可见光与光氧化还原催化相结合的新技术。