ORGANOFLUORINE COMPOUNDS OF BIOLOGICAL INTEREST VIA SELECTIVE FLUORINATIONS

该项目将探索合成途径，以产生 生物活性C-氟代化合物通过选择性 氟化作用。氟与有机体系的结合 通常对人的生物活性有明显的影响 底物。主要焦点将放在亲电材料的使用上。 试剂作为选择性氟化的来源。这些措施包括但 不限于F-TEDA、NFSi和XeF2。化合物的主要类别 将被研究的包括烯烃、芳烃、碳水化合物、N- 杂环、核苷和类固醇。 具体目标包括产生新材料和/或 开发更好的途径来获得已知活性的化合物。至 促进这些定向合成，将努力定义 这些试剂的适用范围，并了解 催化剂对工艺区域选择性的影响。在……里面 除了简单的圆周率键的氟化，共加成 亲核物种，如醇、胺、水、腈、 将对硫醇和碳酸进行研究，以导致 氟烷氧基化等，从而生成氟醚， 氟化醇、氟胺等的氟化途径 芳香族化合物，包括杂环化合物，包括直接和通过芳香族化合物 有机金属学，将被调查。环状氟化经常 大大增强了生物活性。 所使用的方法是以综合和机械为标准的。 有机化学。色谱技术(气相色谱、高效液相色谱和薄层色谱) 将用于化合物的分析、分离和分离。 结构表征将通过光谱学实现 技术(FT-核磁共振、GC-MS、FT-IR、UV-Vis)。新的化合物将是 提供生物活性筛查服务，由 与生物活性评估领域的专家进行安排。

This project will explore synthetic routes to the generation of biologically active C-fluorinated compounds via selective fluorinations. The incorporation of fluorine into an organic system often has a pronounced effect on the biological activity of the substrate. Primary focus will be on the use of electrophilic reagents as the source of selective fluorination. These include but are not limited to F-TEDA, NFSi and XeF2. Key classes of compounds to be studied include alkenes, aromatics, carbohydrates, N- heterocycles, nucleosides and steroids. Specific aims include the generation of new materials and/or the development of better routes to compounds of known activity. To facilitate these directed syntheses, efforts will be made to define the bounds of applicability of these reagents and to learn the effects of catalysts on the regioselectivity of the processes. In addition to simple fluorination of pi bonds, the co-addition of nucleophilic species such as alcohols, amines, water, nitriles, thiols and C-acids will be investigated leading to fluoroalkoxylation, etc. and thus to the generation of fluoroethers, fluoroalcohols, fluoroamines, etc. Routes to the fluorination of aromatics, including heterocycles, both direct and via organometallics, will be investigate. Ring fluorination often greatly enhances bioactivity. The methods used are those standard to synthetic and mechanistic organic chemistry. Chromatographic techniques (GC, HPLC, and TLC) will be used for the analysis, separation and isolation of compounds. Structural characterization will be achieved by spectroscopic techniques (FT-NMR, GC-MS, FT-IR, UV-VIS). New compounds will be offered for biological activity screening to be carried out by arrangement with specialist in the area of bioactivity assessment.