SYNTHESIS OF BIOLOGICALLY ACTIVE CYCLOPENTENONES

具有生物活性的环戊烯酮的合成

• 批准号: 2174682
• 负责人: NEIL E SCHORE
• 金额: $ 11.9万
• 依托单位: UNIVERSITY OF CALIFORNIA AT DAVIS
• 依托单位国家: 美国
• 财政年份: 1993
• 资助国家: 美国
• 起止时间: 1993-09-01 至 1996-08-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/2174682
• 关键词: chemical synthesis; cyclic ketone; cyclopentane

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. Target molecules currently under investigation, and proposed target molecules for future research include quadrone, laurenene, the pentalenolactones, carbacyclins, and hydrazulenes. These molecules display a wide range of biological activity and include antibiotics, cytotoxics and anti-cancer agents, and therapeutic agents for circulatory disorders. The methodology to be used is derived from the organometallic cycloaddition processes which have been highly successful in the past at permitting synthetic schemes to bypass much conventional synthetic methodology. The current state of the art permits prediction of success with considerable confidence. This proven methodology is proposed to be supplemented with several new concepts that, taken together, are aimed at addressing those situations in which the methodology does not succeed satisfactorily, and at modifying the existing procedures to permit ready access in a practical way to the desired target molecules in optically active form. The overriding goal of the proposed research will be to generate methodology derived from unique new combinations of several technologies, to permit access to molecules of biomedical importance in their most biologically active forms, as efficiently as possible from readily available materials.

该建议描述了一个涉及项目的项目的延续 合成含有或源自的生物活性分子的合成 包含环戊酮环系统的分子。靶分子 目前正在研究，并提出了未来的靶标分子 研究包括二极管，劳林烯，养生环酮，carbacyclins， 和夹杂烯。这些分子显示出广泛的生物学 活动并包括抗生素，细胞毒素和抗癌药，以及 循环系统疾病的治疗剂。要使用的方法 是从已经有机金属的环载工过程中得出的 过去，在允许合成方案绕过的情况下非常成功 许多常规的合成方法。当前的艺术状态 允许对成功的预测充满信心。这被证明 建议方法可以补充几个新概念，这些概念，这些概念， 总的来说，旨在解决那些情况 方法论并不令人满意，也无法修改现有的 以实用方式允许访问所需目标的程序 分子以光学活性形式。拟议中的压倒性目标 研究将是生成源自独特的新方法的方法 几种技术的组合，允许访问分子 生物医学在其最活跃的形式中的重要性， 从随时可用的材料中有效地有效。