SYNTHESIS OF MEDIUM RING ANTITUMOR SUBSTANCES

中环抗肿瘤物质的合成

• 批准号: 3278050
• 负责人: ROBERT K BOECKMAN
• 金额: $ 8.4万
• 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: 1982-09-15 至 1986-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3278050
• 关键词: cycloalkene; drug design /synthesis /production

The objectives of this project are the development of synthetic routes to two classes of medium ring natural products exemplified by eremantholide A and the complex diterpenoid taxusin. No efficient synthetic routes to these complex substances are presently known, yet these substances or related derivatives possess marked and promising antitumor activity in a variety of tumor cell lines. The proposed synthetic route to eremantholide A is convergent and features the preparation and coupling of two key optically active fragments. The proposed route to taxusin features the development of a two-carbon ring expansion, and the preparation of the bridgehead olefin by an aldol-dehydration sequence.

该项目的目标是开发合成路线， 两类中环天然产物， 和复合二萜紫杉醇。 没有有效的合成路线 这些复杂的物质是目前已知的，但是这些物质或 相关衍生物具有显著的和有希望的抗肿瘤活性， 多种肿瘤细胞系。 拟合成路线 A是收敛的，其特征在于两个键的制备和耦合， 光学活性碎片。 紫杉醇的拟议路线的特点是， 发展一种双碳扩环，并制备了 桥头烯烃通过羟醛-脱水序列。