Application of new catalytic technologies in the synthesis of substituted piperazines. New approaches for the synthesis of calcium channel blockers for pain treatment.

新型催化技术在取代哌嗪合成中的应用

• 批准号: 365198-2008
• 负责人: Schafer, Laurel
• 金额: $ 3.64万
• 依托单位: University of British Columbia
• 依托单位国家: 加拿大
• 项目类别: Strategic Projects - Group
• 财政年份: 2008
• 资助国家: 加拿大
• 起止时间: 2008-01-01 至 2009-12-31
• 项目状态: 已结题
• 来源: https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=406541
• 关键词: Application; new; catalytic; technologies; synthesis

Catalytic methods afford energy efficient routes for the synthesis of complex molecules. Recent developments from a pharmaceutical company in Vancouver, British Columbia, Neuromed, have shown that a family of nitrogen containing cyclic compounds, piperazines, can be used for a novel approach toward the treatment of chronic pain. Chronic pain affects the lives of millions of Canadians and costs the country billions in reduced productivity and increased medical costs. Consequently, new orally available treatments that avoid addictive and sedative side-effects that are common with drugs such as Morphine, are highly sought after. This proposal addresses an alternative, catalytic synthetic approach for the rapid and facile synthesis of this class of piperazine products. The catalysts to be employed for this reaction build carbon-nitrogen bonds with no by-products and are a new class of catalysts that take advantage of the low cost and low toxicity of zirconium metal. The proposed synthetic strategy reduces the number of synthetic steps, which in turn reduces waste-streams while accessing a broad range of piperazines which may display desirable biological activity. Neuromed pharmaceuticals will be involved in screening catalytically prepared compounds for favourable activity. Overall, the impact of this new synthetic approach will improve manufacturing efficiency and flexbility to enhance productivity while reducing energy consumption and environmental impacts in the synthesis of this important class of compounds.

催化方法为复杂分子的合成提供了能量有效的途径。来自不列颠哥伦比亚省温哥华的一家制药公司Neuromed的最新进展表明，一类含氮环状化合物哌嗪可用于治疗慢性疼痛的新方法。慢性疼痛影响着数百万加拿大人的生活，并使该国的生产力下降和医疗费用增加数十亿美元。因此，避免吗啡等药物常见的成瘾和镇静副作用的新的口服治疗方法受到高度追捧。该建议提出了一种快速简便合成这类哌嗪产品的替代催化合成方法。用于该反应的催化剂建立碳-氮键而没有副产物，并且是利用锆金属的低成本和低毒性的新型催化剂。所提出的合成策略减少了合成步骤的数量，这反过来又减少了废物流，同时获得了广泛的哌嗪，这些哌嗪可以显示出所需的生物活性。神经医学制药公司将参与筛选催化制备的化合物的有利活性。总的来说，这种新的合成方法的影响将提高生产效率和灵活性，以提高生产率，同时减少这类重要化合物合成中的能耗和环境影响。