TOTAL SYNTHESIS OF ANTIBIOTICS

抗生素全合成

• 批准号: 2004404
• 负责人: K. C. NICOLAOU
• 金额: $ 20.44万
• 依托单位: SCRIPPS RESEARCH INSTITUTE, THE
• 依托单位国家: 美国
• 财政年份: 1997
• 资助国家: 美国
• 起止时间: 1997-05-01 至 2001-04-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/2004404
• 关键词: Diels Alder reaction; analog; antibiotics; cyclization; drug design /synthesis /production; drug metabolism; vancomycin

DESCRIPTION: The primary goal of the proposed research is the development of a new synthetic route toward the vancomycin family of antibiotics. Specifically, the total synthesis of balhimycin will employ new versions of known methodology for the preparation of diaryl ether rings using a C2-symmetric triazene substrate. Other noteworthy applications include an intramolecular Diels-Alder addition. Degradation studies of balhimycin are expected to intercept and facilitate the total synthesis at a critical stage and to lead to the preparation of analogs for biological screening against drug resistant bacterial strains.

DESCRIPTION: The primary goal of the proposed research is the development of a new synthetic route toward the vancomycin family of antibiotics. Specifically, the total synthesis of balhimycin will employ new versions of known methodology for the preparation of diaryl ether rings using a C2-symmetric triazene substrate. 其他值得注意的应用包括 intramolecular Diels-Alder addition. Degradation studies of balhimycin are expected to intercept and facilitate the total synthesis at a critical stage and to lead to the preparation of analogs for biological screening against 耐药菌株。