ASYMMETRIC SYNTHESIS OF IONOPHORE & MACROLIDE ANTIBIOTIC

离子载体的不对称合成

• 批准号: 3282901
• 负责人: David A Evans
• 金额: $ 23.09万
• 依托单位: HARVARD UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1983
• 资助国家: 美国
• 起止时间: 1983-08-01 至 1990-11-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3282901
• 关键词: antibiotics; drug design /synthesis /production; drug vehicle; ethers; ion transport; ionophores; macrolide antibiotics; membrane permeability; pharmacokinetics; stereochemistry

The objectives of this proposal are to make creative contributions to the total synthesis of naturally occurring substances possessing clinically significant biological activity. In addition, a number of new reactions are slated for development. The synthesis projects fall into two areas: Antitumor macrolides and polyether antibiotics. The antineoplastic macrolides which will be targets for asymmetric synthesis include both bryostatin and cytovaricin. The two ionophore projects will be concerned with the asymmetric syntheses of ferensimycin-B and lonomycin. New reactions slated for development will include hydroxyl-directed hydrogenations, hydrosilylations, and hydroborations. These reactions should contribute significantly to the development of new concepts and methodology in acyclic stereocontrol.

本提案的目的是为促进《公约》的实施作出创造性贡献。 天然存在的具有临床意义的物质的全合成 重要的生物活性。 此外，一些新的反应 被列入发展计划。 综合项目分为两个领域： 抗肿瘤大环内酯类和聚醚类抗生素。 抗肿瘤 将成为不对称合成目标的大环内酯包括 苔藓抑素和细胞曲张素。 这两个离子载体项目将受到关注 不对称合成费伦西霉素B和洛诺霉素。 新 预定开发的反应将包括羟基导向的 氢化、氢化硅烷化和硼氢化。 这些反应 应大大有助于新概念的发展， 非周期立体控制方法。