Novel Methods for Radical and Electrophilic Amination

化学部的化学合成计划支持由H.Lee Moffitt癌症中心的Justin Lopchuk教授领导的一个项目。他正在开发有机合成的新方法。本项目主要研究碳-氮键的形成。许多重要的化学品，特别是药品、农用化学品和材料，都有碳-氮键。新方法强调了在以前的工作中被忽视的试剂。特别令人感兴趣的是使用具有不寻常电子计数的含氮前驱体。另一类试剂的特点是含有一个或两个氮原子的小环。除了实验室研究，洛普丘克教授还领导了几项努力，以扩大他的工作的影响。他正在组织研讨会，以促进合作，并教育非化学家有机化学和药物化学的价值。含氮化合物在自然界中普遍存在，包括大多数小分子药物以及许多正在开发的药物。在化学系化学合成项目的支持下，H.Lee Moffitt癌症中心的Justin Lopchuk教授正在领导一个项目，以发明碳-氮(C-N)键的新途径。尽管最近取得了相当大的进展，但亲电胺化和自由基胺化仍然具有挑战性，特别是在分子间反应的背景下。这个项目的目标是设计和合成一系列用于所需的亲电或自由基胺化的应变工作台稳定试剂。这些试剂用于一系列不同的反应，并得到多种中间体。目标是快速制备包括胺、联胺和杂环在内的各种高价值含氮化合物。这些成分与药物化学、化学生物学、农业化学和材料科学有关。这项工作的更广泛影响始于为药物发现创建一个新的化合物筛选文库。关于合成有机化学的互动研讨会正在开发中，以促进整个莫菲特癌症中心和南佛罗里达大学的工作人员之间的沟通。这一奖项反映了NSF的法定使命，并通过使用基金会的智力优势和更广泛的影响审查标准进行评估，被认为值得支持。

The Chemical Synthesis Program of the Chemistry Division supports a project led by Professor Justin Lopchuk at the H. Lee Moffitt Cancer Center. He is developing new methods for organic synthesis. This project focuses on the formation carbon-nitrogen bonds. Many important chemicals, especially pharmaceuticals, agrochemicals, and materials, have carbon-nitrogen bonds. The new methods emphasize reagents that have been overlooked in previous work. Of particular interest is the use nitrogen-containing precursors with unusual electron counts. Another class of reagents features small rings containing one or two nitrogen atoms. In addition to the laboratory research, Professor Lopchuk is leading several efforts to broaden the impact of his work. He is organizing workshops to facilitate collaborations and educating nonchemists about the value of organic and medicinal chemistry. Nitrogen-containing compounds are ubiquitous in nature and comprise the majority of small molecule pharmaceuticals as well many of those in development. Supported by the Chemical Synthesis Program of the Chemistry Division, Professor Justin Lopchuk at the H. Lee Moffitt Cancer Center is leading a program to invent new routes to carbon-nitrogen (C-N) bonds. Despite the considerable recent advances, both electrophilic amination and radical amination remain challenging, especially in the context of intermolecular reactions. The goal of this project is the design and synthesis of a series of strained bench-stable reagents for the required electrophilic or radical aminations. These reagents are used in a diverse array of reactions and give versatile intermediates. The goal is the rapid preparation of a wide range of high value nitrogen-containing compounds including amines, hydrazines, and heterocycles. These components are relevant to medicinal chemistry, chemical biology, agrochemistry and materials science. The broader impacts of this work starts with the creation of a novel compound screening library for drug discovery. An interactive workshop on synthetic organic chemistry is being developed to facilitate communication among staff throughout the Moffitt Cancer Center and the University of South Florida.This award reflects NSF's statutory mission and has been deemed worthy of support through evaluation using the Foundation's intellectual merit and broader impacts review criteria.