講師：Frederic R. LEROUX 博士 （University of Strasbourg, France）
講演題目：Fluoraalkyl Amino Reagents (FAR) as Powerful Tool in Organic Synthesis
講演概要：Fluorinated heterocycles are important building block in pharmaceutical and agrochemical sciences and play a key role in modern Crop Protection. Fluoroalkyl- and fluoroalkoxy- groups are popular functional substituents and their introduction can significantly improve biological activity of active ingredients. α,α-Difluoroalkylamines belong to the so-called Fluoroalkyl Amino Reagents (FAR) and can be readily prepared from commercially available fluoro-olefins (monomers used for polymers production) and secondary amines. While these reagents have previously been used only for the replacement of OH with Fluorine in alcohols and carboxylic acids, we recently became interested in their use to prepare fluoroalkyl-containing heterocycles. It has been demonstrated that FARs, after activation with Lewis acids such as BF3 and AlCl3, afford iminium salts with Vilsmeier-type activity with “unexhausted” potential for further transformations. We have exploited their reactivity to prepare diversity of fluorinated pyrazoles, isoxazoles, pyrimidines, quinolines, which are important building blocks for numerous modern agrochemicals.