Synthesis of deuterium labelled compounds for potential use in pain therapy

合成可用于疼痛治疗的氘标记化合物

• 批准号: 485272-2015
• 负责人: Snieckus, Victor
• 金额: $ 1.82万
• 依托单位: Queen's University
• 依托单位国家: 加拿大
• 项目类别: Engage Grants Program
• 财政年份: 2015
• 资助国家: 加拿大
• 起止时间: 2015-01-01 至 2016-12-31
• 项目状态: 已结题
• 来源: https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=584834
• 关键词: Synthesis; deuterium; labelled; compounds; potential

Before the synthesis of urea in 1828, organic molecules were available only through biological processes. Continuous advances in the chemical sciences has led to development of methods that can be used for the design and synthesis of complex molecules. Many of these synthetic molecules have found wide range of applications including as crop protection agents, cosmetics, food preservatives and medicines. Among several classes of synthetic molecules, deuterated medicinal compounds are of extraordinary interest due to their applications as modern pharmaceutical agents. However, their methods of preparation are challenging and require expensive starting materials. For this reason, there has been special interest in developing new methods for the synthesis of deuterated medicinal compounds for testing against new diseases or for many other biological studies. Through this proposal, we plan to develop efficient synthetic methodologies to prepare biologically important deuterated pharmaceutical compounds (e.g. Silodosin, Canagliflozen, Ledipasvir, Vilazodone) for their use in the pharmaceutical industry. Previous methods such as the directed ortho metalation (DoM) reaction, 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 less expensive drugs and hence provide health and economic benefits to Canadians. Through this work we will also train highly qualified workers for the Canadian labour market.

在1828年合成尿素之前，有机分子只能通过生物过程获得。 化学科学的不断进步已经导致了可用于化学分析的方法的发展。 复杂分子的设计和合成。许多这些合成分子已经发现了广泛的 应用包括作为作物保护剂、化妆品、食品防腐剂和药物。在几个 作为一类合成分子，氘代药用化合物由于其 作为现代医药的应用。然而，它们的制备方法具有挑战性， 需要昂贵的起始材料。由于这个原因，人们对开发新方法特别感兴趣 用于合成氘代药用化合物，用于测试对抗新疾病或用于许多其它疾病， 生物学研究。通过这一提议，我们计划开发有效的合成方法来制备 生物学上重要的氘代药物化合物（例如Silodosin，Canagliflozen，Ledipasvir， 维拉唑酮）用于制药工业。以前的方法，如定向正交 金属化（DoM）反应，在我们的实验室发现和发展，正在使用的制药 工业（如孟山都、辉瑞、百时美施贵宝、默克）用于多公斤药物的商业生产， 农用化学品和其他商品化学品。这项研究提案旨在帮助生产更便宜的 药物，从而为加拿大人提供健康和经济利益。通过这项工作，我们还将培训 为加拿大劳动力市场提供高素质的工人。