SYNTHETIC STUDIES TOWARDS TAXOL AND RELATED COMPOUNDS

本研究的主要目的是使 通过合成研究对有机化学和医学的贡献 对紫杉烷类天然产品，特别是集中在 抗肿瘤生物碱紫杉醇 我们的研究工作将集中在 开发一个实用的，通用的，灵活的全合成， 紫杉醇用于两个目的：（1）确保紫杉醇的大规模供应， 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/活性研究的多种紫杉醇类似物， 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建紫杉醇的环B， 使用Ni（II）/Cr（II）介导的偶联反应， 逐步的方式。这种方法的明显优点包括： 收敛程度和灵活性以及最少的步骤 键耦合后官能团操作所需的 反应 通过使用一个模型系统，我们已经证明了可行性 这种方法。

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.