SYNTHESIS OF BIOLOGICALLY ACTIVE HETEROCYCLES AND PROSTA

一些具有潜在重要意义的杂环化合物的新合成路线 化合物，包括呋喃，丁烯内酯，苯并呋喃，色烯， 香豆素、异香豆素、β-内酰胺、特特拉姆酸、吡咯、吲哚， 喹啉、异喹啉和苯并二氮杂。 这些 杂环广泛存在于自然界中，并表现出显著的生理活性 活动 它们已被发现用于治疗癌症、循环系统疾病和 心脏病，细菌和真菌感染。 广泛的 在这些化合物中，抗生素活性是明显的。 我们以前的工作 有机金属化合物的新的合成应用已经提出了一个 许多新颖的新方法，这些环系统，所有这些都需要 有机钯化合物易于制备的优点 从有机汞或铊化合物或通过直接钯化 乙炔和芳香族化合物，和设施， 有机钯化合物与一氧化碳或烯烃反应， 新的碳碳键 职能组的适当定位 应该允许新的新的合成所提到的杂环系统 以上 这项工作的顺利完成，应（1）开辟全新的 这些天然存在的、具有生物活性的杂环的途径，（2） 提供了许多有趣的新化合物， 显示出生理活性和希望的药用价值， (3)简化了这些极其重要杂环的许多合成。

A number of potentially important new synthetic routes to heterocyclic compounds, including furans, butenolides, benzofurans, chromenes, coumarins, isocoumarins, Beta-lactams, tetramic acids, pyrroles, indoles, quinolines, isoquinolines and benzodiazepines, are outlined. These heterocycles occur widely in nature and exhibit substantial physiological activity. They have found use in the treatment of cancer, circulatory and heart ailments, and bacterial and fungal infections. A broad spectrum of antibiotic activity is evident among these compounds. Our previous work on new synthetic applications of organometallic compounds has suggested a number of novel new approaches to these ring systems, all of which take advantage of the ease with which organopalladium compounds can be prepared from either organomercury or -thallium compounds or via direct palladation of acetylenes and aromatic compounds, and the facility with which organopalladium compounds react with carbon monoxide or olefins to generate new carbon-carbon bonds. The appropriate positioning of functional groups should allow novel new syntheses of the heterocyclic ring systems mentioned above. Successful completion of this work shold (1) open up entirely new routes to these naturally occurring, biologically active heterocycles, (2) provide a number of interesting new compounds which might be expected to show physiological activity and hopefully medicinal utility, and finally (3) simplify many a synthesis of these vitally important heterocycles.