NOVEL ASYMMETRIC SYNTHESIS OF ANTI-AIDS COMPOUNDS

本研究计划的主要目标是 提案都是制定和执行效率不对称的 天然产物中结构类型的合成 蓖麻黄素、脱氧诺吉霉素和其他葡萄糖苷酶抑制剂，以及 氧杂环辛酸--一种新型的含氧杂环己烷的反向核苷 转录酶抑制活性。这些结构上截然不同的成员 各类化合物正受到密切关注，因为它们的反 人类免疫缺陷病毒(HIV)活性。 虽然我们用天然化合物的合成来说明我们的策略， 我们主要关注的是合成路线的定义 足够普遍以至于可以直接进行类似物的合成， 无需重新设计每个新的合成协议 衍生品。因此，我们预计我们的合成材料的通用性 这些方法将使新分子的生产变得容易 在结构上与目标化合物(即类似物)相关，从而 使人们能够更好地理解化学物质之间的关系 建筑和生物功能。某些模拟合成是 在本提案中讨论的。

The principle objectives of the research program as set forth in this proposal are the development and execution of efficient asymmetric syntheses of the structural types found in the natural products castanospermine, deoxynojirimycin, and other glucosidase inhibitors, and oxetanocin, a novel oxetane-containing nucleosides with reverse transcriptase inhibitory activity. Members of these structurally distinct classes of compounds are being intensely scrutinized because of their anti- human immunodeficiency virus (HIV) activity. While we illustrate our strategy with syntheses of the natural compounds, our primary concern is with the definition of synthetic routes that are general enough so that the synthesis of analogs can be pursued directly, without the need to redesign the synthetic protocol for each new derivative. Thus, we expect that the generality of our synthetic approaches will allow for the facile production of new molecules structurally related to the target compounds (i.e., analogs), thereby enabling a better understanding of the relationship of chemical architecture and biological function. Certain analog syntheses are discussed in this proposal.