THE SYNTHESIS OF ROSARAMYCIN AND RELATED SYSTEMS

玫瑰霉素的合成及相关系统

• 批准号: 3128530
• 负责人: RICHARD H SCHLESSINGER
• 金额: $ 11.47万
• 依托单位: UNIVERSITY OF ROCHESTER
• 依托单位国家: 美国
• 财政年份: 1982
• 资助国家: 美国
• 起止时间: 1982-09-30 至 1988-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3128530
• 关键词: anaerobic bacteria; antibacterial agents; antibiotics; drug design /synthesis /production; erythromycin; glucose; gram negative bacteria; gram positive bacteria; lactones; macrolide antibiotics; malates

The specific aims of this grant include two total syntheses which are based on aldol chemistry developed in these laboratories three years ago. This methodology utilizes the chemistry of enolate systems arising from vinylogous urethanes. The first of these synthetic targets is the macrolide antibiotic rosaramycin (1), a molecular system of considerable biological interest. Our synthetic effort on this molecule is in its third year. The progress report and first part of the experimental design and methods section of this proposal will discuss the current status of this problem and our intended future efforts on it, respectively. The second part of this proposal involves a construction of the seco-acid of erythromycin (2). In this section, we will propose a detailed study of the methodology we intend to employ for the synthesis along with a description of the synthetic route itself.

这笔赠款的具体目标包括两个完全合成，它们是基于 关于三年前在这些实验室开发的Aldol化学。这 方法学利用产生的烯烃体系的化学 乙烯基氨基甲酸酯。这些合成目标中的第一个是 大环内酯类抗生素罗沙霉素(1)，一个相当大的分子体系 生物兴趣。我们对这种分子的合成工作已进入第三阶段。 年。进度报告和实验设计的第一部分和 本建议书的方法部分将讨论此方法的现状 问题和我们未来在这个问题上的打算。 该提案的第二部分涉及第二酸的建造。 红霉素(2)。在这一部分中，我们将建议详细研究 我们打算采用的合成方法以及一个 合成路线本身的描述。