ORGANOFLUORINE COMPOUNDS OF BIOLOGICAL INTEREST VIA SELECTIVE FLUORINATIONS

该项目将探索合成路线， 生物活性碳氟化合物通过选择性 氟化 将氟掺入有机体系中 通常对生物活性有显著的影响， 衬底 主要重点将是使用亲电 试剂作为选择性氧化的来源。 这些包括但 不限于F-TEDA、NFSi和XeF 2。 主要化合物类别 要研究的包括烯烃、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 开发获得已知活性化合物的更好途径。 到 为了促进这些定向合成，将努力定义 这些试剂的适用范围，并了解 催化剂对方法的区域选择性的影响。 在 除了简单的π键外， 亲核物质如醇，胺，水，腈， 硫醇和C-酸将进行研究， 氟烷氧基化等，并因此产生氟代醚， 氟代醇、氟代胺等。 芳族化合物，包括杂环，直接和经由 有机金属，将进行调查。 经常打电话 大大提高了生物活性。 所使用的方法是那些标准的合成和机械 有机化学 色谱技术（GC、HPLC和TLC） 将用于化合物的分析、分离和离析。 将通过光谱法进行结构表征 技术（FT-NMR、GC-MS、FT-IR、UV-VIS）。 新化合物将 用于生物活性筛选， 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.