SYNTHETIC STUDIES TOWARDS TAXOL AND RELATED COMPOUNDS

这项研究的主要目的是使有意义的 通过合成研究对有机化学和医学的贡献 紫杉烷类天然产品，特别侧重于 抗肿瘤生物碱紫杉醇。我们的研究工作将集中在 一种实用、通用、灵活的全合成方法的研制 紫杉醇用于两个目的：(1)确保紫杉醇的大规模供应或 临床使用的最有效的紫杉醇类似物和(2)提供一种 用于结构/活性研究的紫杉醇类似物种类繁多 以确定最有效的紫杉醇类似物。在实验中，我们计划 在合成的最后阶段构筑紫杉醇的B环 利用Ni(II)/Cr(Il)介导的偶联反应同时或 循序渐进的方式。这种方法的明显优势包括 收敛程度和灵活性以及最低步骤数 键连接后的功能组操作所需 反应。通过一个模型系统，验证了该方法的可行性。 这种方法的一部分。

The major objective of this research is to make significant contributions to organic chemistry and medicine through synthetic studies towards the taxane class of natural products, specifically focused on the antitumor alkaloid taxol. Our research efforts will be focused on the development of a practical, general, and flexible total synthesis of taxol for two purposes: (1) to secure a large scale supply of taxol or the most effective taxol analogue for clinical use and (2) to provide a wide variety of taxol analogues for structure/activity studies in order to identify the most effective taxol analogue. Experimentally, we plan to construct the ring B of taxol at the very late stage of synthesis by using the Ni(II)/Cr(Il)-mediated coupling reaction in a simultaneous or step-wise manner. Obvious advantages of this approach include a high degree of convergence and flexibility and a minimum number of steps required for the functional group manipulation after the key coupling reaction. By using a model system, we have demonstrated the feasibility of this approach.