CHIRAL APPROACHES TO NATURAL PRODUCTS SYNTHESIS

描述：(首席调查员)这项工作的长期目标 项目包括复杂天然产物的实验室合成 具有良好的生物活性以及开发新的 综合方法论将简化这项任务。特效天然 待研究的产品包括前景看好的抗癌药物根霉毒素， 结构简单的根霉毒素类似物，以及高度细胞毒性的 海洋天然产物Swinholide以及米沙激动素和镰刀菌素C， 这两种药物在结构上都与Swinholide非常相似。此外, 针对Epothilone A&B和Bryostatin 1的整体合成的研究将 被启动。埃博西酮是一种令人兴奋的生物新药。 活性与紫杉醇非常相似，因此是紫杉醇的重要新结构 与癌症化疗的相关性。强效新型免疫抑制剂 皮洛尼汀也将被合成。该计划的主旨是从一个 从化学的角度来看，是开发新的策略和反应 简化这些材料的合成。这是一个重要的焦点 研究人员正在开发催化不对称反应，使 通过两个sp2中心的结合形成新的立体中心 由催化剂控制的方式。

DESCRIPTION: (Principal Investigator's) The long term objectives of this program include the laboratory synthesis of complex natural products possessin desirable biological activity as well as the development of new synthetic methodology which will simplify this task. Specific natural products to be studied include the promising antitumor agent rhizoxin, structurally simplifie analogues of rhizoxin, and the highly cytotoxic marine natural product swinholide as well as misakinolide and scytophycin C, both of which are structurally very similar to swinholide. In addition, studies directed at tota syntheses of epothilone A & B and bryostatin 1 will be initiated. The epothilones are exciting new agents with biological activity very similar to taxol, and are thus important new structures of relevance to cancer chemotherapy. The potent new immunosuppressive agent pironetin will also be synthesized. The main thrust of the program, from a chemical point of view, is to develop new strategies and reactions which simplify the synthesis of these materials. An important focus of this research is the development of catalytic asymmetric reactions which allow for the formation of new stereogenic centers via union of two sp2 centers in a manner controlled by the catalyst.