ASYMMETRIC SYNTHESIS OF IONOPHORE/MACROLIDE ANTIBIOTICS

这项拟议的研究的目标是使创造性 对天然物质总合成的贡献 具有临床意义的生物活性的。这笔赠款将 继续处理新的立体选择性反应的发展和 该方法学在不对称合成中的应用 聚乙酸酯和聚丙酸类抗生素和抗肿瘤药物 探员们。合成靶标将包括抗肿瘤药物 天然产物Bryostatin、Neristatin、Miyakolide、Spasgistatin和 缩水甘油。聚丙酸酯衍生的大环内酯类抗生素将是 合成的药物包括兰卡霉素和兰卡霉素。 处理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 预测复杂的羟醛过程的立体化学过程。目标是 这些研究将揭示出一些普遍的规律 预测复杂的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.