ASYMMETRIC SYNTHESIS OF IONOPHORE/MACROLIDE ANTIBIOTICS

这项研究的目的是创造性地 对天然物质全合成的贡献 具有临床显著的生物活性。这笔赠款将 继续开发新的立体选择性反应， 该方法在不对称合成中的应用 聚乙酸酯和聚丙酸酯衍生的抗生素和抗生素 剂.合成目标将包括海军陆战队 天然产物苔藓抑素，neristatin，miyakastatin，spongistatin， altohyrtin。聚丙酸衍生的大环内酯类抗生素， 合成的抗生素包括竹桃霉素和兰卡霉素。 新反应发现的方法学研究将 强调反应的发展，以控制和最终 预测复杂羟醛缩合过程的立体化学过程。目标 这些研究将揭示一些一般规则， 预测复杂羟醛片段偶联的立体化学结果 反应.

The objectives of this proposed research are to make creative contributions to the total synthesis of naturally occurring substances possessing clinically significant biological activity. This grant will continue to address the development of new stereoselective reactions and the application of this methodology to the asymmetric synthesis of polyacetate and polypropionate-derived antibiotics and antineoplastic agents. The synthesis targets will include the antineoplastic marine natural products bryostatin, neristatin, miyakolide, spongistatin, and altohyrtin. Polypropionate-derived macrolide antibiotics that will be synthesized include oleandomycin and lankamycin. The methodological studies dealing with new reaction discovery will emphasize the development of reactions for controlling and ultimately predicting the stereochemical course of complex aldol processes. The goal of these studies will be to reveal some of the general rules for predicting the stereochemical outcome of complex aldol fragment coupling reactions.