NEW HIGHLY EFFICIENT ROUTES TO POLYKETIDES

生产聚酮的高效新途径

• 批准号: 6196383
• 负责人: Michael Arthur Calter
• 金额: $ 10.19万
• 依托单位: UNIVERSITY OF ROCHESTER
• 依托单位国家: 美国
• 财政年份: 1997
• 资助国家: 美国
• 起止时间: 1997-12-15 至 2002-11-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/6196383
• 关键词: antibiotics; biological products; carboxylate; drug design /synthesis /production; polymers

DESCRIPTION: (Principal Investigator's) The goal of this project is to develop inexpensive methods for making large amounts of useful drugs. The particular class of compounds that are the focus of this project are the polyketides. These molecules are widely used in clinical practice, particularly as antibiotics. For example, erythromycin is a complex polyketide that has found wide use as an antibiotic, because of its ability to kill bacteria without affecting humans. Physicians use other polyketides as antiviral, antifungal, anticancer and immunosuppressive agents. Although methods do exist for the synthesis of polyketides, the methods described in this proposal are much more applicable to industrial use than existing ones. The most important way in which the proposed chemistry differs from current methods is in the use of a catalytic reaction to prepare the starting materials. Only very small amounts of the catalyst are required in the proposed methods, and it is likely that the catalyst will be reused time and time again. Another advantage of the proposed chemistry is that a number of steps can be run in the same reaction solvent and reactor. This property is very important for industrial syntheses, as each additional solvent and reactor increases the amount of waste and complexity of the process.

描述：（主要调查员）该项目的目的是 开发廉价的方法来制作大量有用的药物。 这 该项目重点的特定化合物是 聚酮化合物。 这些分子广泛用于临床实践， 特别是作为抗生素。 例如，红霉素是一个复杂的 由于其能力 杀死细菌而不会影响人类。 医师使用其他聚酮化合物 作为抗病毒，抗真菌，抗癌和免疫抑制剂。 尽管确实存在合成聚酮化合物的方法，但方法 本提案中描述的更适用于工业用途 现有的。 提出的化学的最重要方法 与当前方法不同是使用催化反应 准备起始材料。 只有很少的催化剂是 在提议的方法中需要，催化剂可能是 一次又一次地重复使用。 提出的化学的另一个优点是 可以在相同的反应溶剂和反应器中运行多个步骤。 该属性对于工业合成非常重要，因为每增加一次 溶剂和反应堆增加了废物的量和复杂性 过程。