ALKYNYLIODONIUM CHEMISTRY IN ORGANIC SYNTHESIS

炔基碘鎓盐的开发与应用 将进行立体选择性有机合成。 这些试剂 显示出独特的反应模式， 结构容易从简单的无环前体组装。 在 特别地，含氮粘合剂与这些盐的使用将 导致几个分子框架的有效构建， 药学上感兴趣的生物碱，包括 三尖杉属植物群，以及弹力蛋白A、麦哲伦酮和 帕劳胺。 这些目标结构中的几个（例如， 脱氧三尖杉酯碱，agelastatin A）显示非常有前途的抗白血病 和抗氧化活性， 免疫调节反应。 及时获取这些生物活性靶标 通过炔基碘鎓盐方法将有助于 了解它们的作用机制，并将提供 用于进一步优化/评价生物活性的结构。

The development and exploitation of alkynyliodonium salts for stereoselective organic synthesis will be pursued. These reagents display unique reactivity patterns which permit polycyclic chemical structures to be assembled readily from simple acyclic precursors. In particular, the use of nitrogen-containing addends with these salts will lead to efficient construction of the molecular framework of several pharmaceutically interesting alkaloids including members of the Cephalotaxus group, as well as agelastatin A, magellaninone, and palau'amine. Several of these target structures (e.g., deoxyharringtonine, agelastatin A) display very promising antileukemic and antineoplastic activity, while palau'amine elicits an immunomodulatory response. Timely acquisition of these bioactive targets through alkynyliodonium salt methodology will contribute to an understanding of their mechanism of action and will provide lead structures for further optimization/evaluation of biological activity.