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Alternatives to palladium catalysis for the elaboration of nitrogen heterocycles

用于合成氮杂环的钯催化替代品

基本信息

批准号：
459118-2013
负责人：
Snieckus, Victor
金额：
$ 7.6万
依托单位：
Queen's University
依托单位国家：
加拿大
项目类别：
Collaborative Research and Development Grants
财政年份：
2014
资助国家：
加拿大
起止时间：
2014-01-01 至 2015-12-31
项目状态：
已结题

来源：
https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=555479
关键词：
Alternatives palladium catalysis elaboration nitrogen

项目摘要

Prior to the development of synthetic organic chemistry, organic compounds were accessible only through natural biological processes. With the advancement of the chemical sciences especially since the 1950s, molecules of great complexity can now be readily synthesized providing medicines and crop protection agents for the benefit of humankind. Currently, palladium-catalyzed bond forming reactions are one of the most popular techniques used by synthetic chemists to prepare desired organic compounds, including pharmaceutically important heteroaromatic derivatives which constitute 80% of today's antibiotics, anticancer, anti-inflammatory and other medicinal agents. Although palladium-mediated methods have become a widely used synthetic tool, palladium metal is expensive and can be difficult to remove from the synthetic steps involved in drug preparation. Through this proposal, we aim to find alternative methods to synthesize heteroaromatic compounds for their use in the pharmaceutical and chemical industry. Previous methods discovered and developed in our laboratories are being used by the pharmaceutical industry (e.g. Monsanto, Pfizer, BMS, Merck) for the multikilogram commercial production of drugs, agrochemicals, and other commodity chemicals. This research proposal aims to help produce methods to make less expensive drugs and hence provide health and economic benefits to Canadians and, in the process, train highly qualified workers for the Canadian labour market.

在合成有机化学发展之前，有机化合物只能通过自然生物过程获得。随着化学科学的进步，特别是自20世纪50年代以来，非常复杂的分子现在可以很容易地合成，为人类提供药物和作物保护剂。目前，钯催化成键反应是合成化学家用来制备所需有机化合物的最常用技术之一，包括具有重要药学意义的杂芳香衍生物，它构成了今天80%的抗生素、抗癌、抗炎和其他药物制剂。虽然钯介导的方法已成为一种广泛使用的合成工具，但钯金属价格昂贵，并且难以从药物制备的合成步骤中去除。通过这一提议，我们的目的是寻找替代的方法来合成杂芳香族化合物，用于制药和化学工业。以前在我们实验室发现和开发的方法正在被制药行业（如孟山都、辉瑞、BMS、默克）用于药品、农用化学品和其他商品化学品的多公斤商业生产。这项研究建议的目的是帮助找到方法，使药品价格更便宜，从而为加拿大人提供健康和经济利益，并在此过程中为加拿大劳动力市场培训高素质的工人。