Application and Development of New Radical Synthetic Methods

该提案的重点是制药和农化工业感兴趣的分子合成新技术的发展。一个关键目标是开发将氟掺入药物的新方法。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重要组成部分。目前，超过20%的畅销药剂含有氟。虽然氟在医学上是有用的，但通常很难将其纳入分子中。本提案的第一和第二部分侧重于利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，包括紫外线。我们还将研究利用更环保和低能耗的可见光与光氧化还原催化相结合的新技术。

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.