SYNTHESIS OF BIOLOGICALLY ACTIVE CYCLOPENTENONES

具有生物活性的环戊烯酮的合成

• 批准号: 3273781
• 负责人: NEIL E SCHORE
• 金额: $ 8.01万
• 依托单位: UNIVERSITY OF CALIFORNIA AT DAVIS
• 依托单位国家: 美国
• 财政年份: 1979
• 资助国家: 美国
• 起止时间: 1979-04-01 至 1990-06-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3273781
• 关键词: antiviral agents; carbonyl compound; cytotoxicity; drug design /synthesis /production; drug screening /evaluation; prostaglandin analogs

This proposal describes the continuation of a project that involves the synthesis of biologically active molecules containing, or derived from molecules containing the cyclopentenone ring system. During the current grant period we have greatly expanded both the scope and our mechanistic knowledge of the organometallic reaction utilizing dicobalt octacarbonyl to promote cocyclization of alkenes, alkynes, and carbon monoxide. A number of synthesis that are either completed or in progress illustrate the enormous power of this method in bypassing conventional routes to molecules containing this ring system. Proposed target molecules for future research include triquinane- derived systems, guaianolides and pseudoguaianolides, and heterocycles, including terpene alkaloid. These materials display a wide range of biological activity and include antibiotics, antiviral, cytotoxics, and anti-cancer agents. The proposed work is designed to further critically test the limits of this methodology, as well as to make available new synthetic routes to these important classes of compounds, routes that involve a minimal number of reaction steps from inexpensive and readily available starting materials.

该提案描述了一个涉及的项目的延续 含有或 源自包含环戊酮环的分子 系统。 在当前的赠款期间，我们有很大的 扩大了范围和我们对 利用二核八核的有机金属反应 促进烷烃，炔烃和一氧化碳的环环化。 许多完成或正在进行的合成 说明了这种方法在绕过的巨大力量 通往包含此环系统的分子的常规路线。 未来研究的拟议靶标分子包括三喹烷 - 衍生系统，瓜伊亚诺德斯和伪藻烷酚以及 杂环，包括萜烯生物碱。 这些材料显示 广泛的生物学活性，包括抗生素， 抗病毒，细胞毒素和抗癌药。 拟议的工作 旨在进一步批判性地测试该限制 方法论，以及提供新的合成路线 这些重要类的化合物，涉及的路线 廉价和容易的反应步骤数量最少 可用的起始材料。