Asymmetric Synthesis of Macrolide Antibiotics

大环内酯类抗生素的不对称合成

• 批准号: 6785496
• 负责人: JAMES L LEIGHTON
• 金额: $ 32.13万
• 依托单位: COLUMBIA UNIV NEW YORK MORNINGSIDE
• 依托单位国家: 美国
• 财政年份: 1998
• 资助国家: 美国
• 起止时间: 1998-08-01 至 2006-07-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6785496
• 关键词: carbonyl group; catalyst; drug design /synthesis /production; macrolide antibiotics; stereochemistry

DESCRIPTION (provided by applicant): This proposal details the development of new, catalytic reaction methodology for the efficient asymmetric synthesis of polyacetate- and polypropionate-derived macrolide antibiotics, It has been documented that drug-resistant bacterial and fungal infections represent a problem of rapidly growing importance. More than simply achieving syntheses of such compounds, the focus of the proposal is on advancing the frontiers of efficiency, waste-minimization and economic viability of such synthetic efforts. The ultimate goal is thus the realization of practicable and practical chemistry that will affect both the discovery and process phases of research into new medicinal agents. This proposal addresses both the continuation and further development of the most promising discoveries made in the previous funding period, as well as exciting new directions only recently initiated. The reactions under study have as their unifying theme tandem reaction methodology. Tandem reactions are inherently more efficient as multiple chemical transformations may be accomplished, and multiple stereogenic centers may be established in a single operation. In this fashion, large segments of the target natural products may be synthesized with unprecedented efficiency employing only readily available and environmentally benign reagents.

描述（由申请人提供）：该提案详细介绍了用于高效非对称合成聚乙酸酯和聚丙酸酯衍生大环内酯类抗生素的新型催化反应方法的发展。已有文献记载，耐药细菌和真菌感染是一个日益重要的问题。这一建议的重点不仅仅是实现这些化合物的合成，而是在提高效率、尽量减少废物和这种合成努力的经济可行性方面取得进展。因此，最终目标是实现实际可行的化学，这将影响新药物研究的发现和过程阶段。