BRIDGEHEAD INTERMEDIATES IN SYNTHESIS

合成中的桥头中间体

• 批准号: 3283518
• 负责人: GEORGE A KRAUS
• 金额: $ 10.01万
• 依托单位: IOWA STATE UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1985
• 资助国家: 美国
• 起止时间: 1985-09-01 至 1992-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3283518
• 关键词: alkenes; bridged cyclic compound; cations; colchicine; cyclic compound; drug design /synthesis /production; lactones; microtubules; sesquiterpenes

The overall goal is to understand the chemistry of bridgehead intermediates and to apply this knowledge to the total synthesis of natural products. The specific goals include 1) the synthesis of the potent antitumor agent shikodonin; 2) the synthesis of colchicine and a heteroatom analog. Colchicine is an inhibitor of mitosis by affecting the action of microtubules; 3) the study of a rearrangement of a bridged ring system to a fused bicyclo(3.3.0) ring system. An immediate application is the antibiotic pentalenolactone E; and 4) the study of the cycloadditions of bridgehead enals with electron-rich alkenes. An immediate application is the isocedrene class of sesquiterpenes.

总体目标是了解桥头堡的化学成分。 并将这一知识应用于全合成 天然产品。具体目标包括1)合成 强效抗癌药物紫草素；2)合成 秋水仙碱和杂原子类似物。秋水仙碱是一种抗癌药物 影响微管活动的有丝分裂；3)一种 桥接环路系统改装成熔融自行车(3.3.0) 振铃系统。一个直接的应用是抗生素 4)环加成反应的研究 桥头烯带有富含电子的烯烃。一个即刻的 用途是倍半萜的异戊二烯类化合物。