STEREOSELECTIVE SYNTHESIS OF CYCLIC ETHERS

描述：该提案的目的是应用小说 分子内酰基自由基环化反应生物合成 重要的环醚。尽管存在多种合成方法 在这些化合物中，寻找具有更多骨架和 立体化学的灵活性仍在继续。酰基自由基已经收到 在有机合成中作为活性中间体的关注相对有限， 尽管它们有可能有效地形成碳-碳键。少年派的 初步的综合研究表明，这种方法很可能会 对目标定向合成具有重要的实用价值。 本文建议的综合研究将集中在制备 顺式-库默斯因、库马斯兰和制定可行的战略 有效的抗真菌药物伽贝酸A-D。藤黄酸A-D 代表已知的最有效的抗真菌药物，其活性超过 两性霉素B增加了三个数量级以上，使它们 极其重要的目标。

DESCRIPTION: The aim of the proposal is the application of novel intramolecular acyl radical cyclizations to the synthesis of biologically important cyclic ethers. Although numerous methods exist for the synthesis of these compounds, the search for new methods with increased skeletal and stereochemical flexibility continues. Acyl radicals have received relatively limited attention as reactive intermediates in organic synthesis, despite their potential to efficiently form carbon-carbon bonds. The PI's preliminary synthetic studies indicate that this methodology is likely to have significant utility for target directed synthesis. The synthetic studies proposed herein will focus on the preparation of cis-kumausyne, kumausallene, and the development of a viable strategy for the potent antifungal agents gamberic acids A-D. The gamberic acids A-D represent the most potent antifungal agents known, with activity exceeding that of amphotericin B by over three orders of magnitude, making them extremely important targets.