ALKYNYLIODONIUM CHEMISTRY IN ORGANIC SYNTHESIS

乙炔基碘盐的开发利用 立体选择性有机合成将是今后的发展方向。这些试剂 显示独特的反应性模式，允许多环化学物质 易于由简单的非环前驱体组装的结构。在……里面 特别是，将含氮添加剂与这些盐一起使用将 导致有效地构建了几个 具有药用价值的生物碱，包括 三尖杉属，以及琼脂糖抑素A、麦哲罗酮和 帕劳阿明。这些目标结构中的几个(例如， 脱氧三尖杉酯碱，Aagelastatin A)显示出非常有希望的抗白血病作用 和抗肿瘤活性，而帕劳胺引起了 免疫调节反应。及时获得这些生物活性靶点 通过烷基碘盐方法学将有助于 了解他们的行动机制，并将提供线索 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.