Synthesis of nitrogen-containing molecules using bifunctional reagents and organocatalysts

使用双功能试剂和有机催化剂合成含氮分子

• 批准号: 311911-2011
• 负责人: Beauchemin, André
• 金额: $ 5.1万
• 依托单位: University of Ottawa
• 依托单位国家: 加拿大
• 项目类别: Discovery Grants Program - Individual
• 财政年份: 2012
• 资助国家: 加拿大
• 起止时间: 2012-01-01 至 2013-12-31
• 项目状态: 已结题
• 来源: https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=514866
• 关键词: Synthesis; nitrogen; containing; molecules; using

Over 90% of the compounds manufactured and tested by pharmaceutical companies have at least one nitrogen atom in their structure, and approximately one reaction out of six performed in the pharmaceutical industry involves the formation of a carbon-nitrogen bond. As such, new methods to access nitrogen containing molecules can help in drug discovery by providing shorter and more efficient access to these compounds. Many fine and bulk chemicals also incorporate nitrogen atoms. Surprisingly, the conversion of cheap petrochemicals or easily accessible starting materials (alkenes, alkynes and arenes) into nitrogen-containing molecules currently requires several steps and more cost-effective, efficient processes are possible and needed. Such direct processes stand out as highly desirable but remain rarely used in industry and academia, despite well-recognized potential and intense research efforts worldwide. This proposal will provide such new technology targeting common structural elements founds in pharmaceuticals and bioactive natural products.

超过90%的制药公司生产和测试的化合物在其结构中至少有一个氮原子，制药行业中进行的六个反应中约有一个涉及碳-氮键的形成。因此，获取含氮分子的新方法可以通过提供更短和更有效的获取这些化合物来帮助药物发现。许多精细和散装化学品也含有氮原子。令人惊讶的是，将廉价的石油化学品或容易获得的起始材料（烯烃、炔烃和芳烃）转化为含氮分子目前需要几个步骤，并且更有成本效益的、有效的方法是可能的和需要的。这种直接方法非常理想，但在工业和学术界仍然很少使用，尽管全世界都在进行广泛的研究和广泛的研究。该提案将提供针对药物和生物活性天然产物中常见结构元件的新技术。