Exploration of new chemicals to enable rapid functionalization of pharmaceuticals**

探索新化学品以实现药物的快速功能化**

• 批准号: 537314-2018
• 负责人: Li, ChaoJun
• 金额: $ 1.82万
• 依托单位: McGill University
• 依托单位国家: 加拿大
• 项目类别: Engage Grants Program
• 财政年份: 2018
• 资助国家: 加拿大
• 起止时间: 2018-01-01 至 2019-12-31
• 项目状态: 已结题
• 来源: https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=657424
• 关键词: Exploration; new; chemicals; enable; rapid

Paraza Pharma intends to diversify pharmaceutical molecules/intermediates for rapid Structure-Activity-Relationship (SAR) studies. However, the current methodologies lacks the compatibility of many functional groups which usually exist in advance pharmaceutical intermediate. Furthermore, many pharmaceutical interesting fragments requires multiple steps to be introduced into the pharmaceutical intermediates. The proposed project will address this problem using novel alkylating reactions recently discovered in Professor Chao-Jun Li's laboratory. The project will pursue new chemical matters which will allow the functionalization of advance pharmaceuticals in one step. The research will be focusing on optimizing reaction conditions to allow chemo-selective and functional group tolerable transformation possible. ****The success of this proposed project will be a significant advancement in pharmaceutical industry research and development.**

帕拉扎制药公司打算使快速构效关系（SAR）研究的药物分子/中间体多样化。然而，目前的方法缺乏对许多功能基团的兼容性，这些功能基团通常存在于高级药物中间体中。 此外，许多药学上感兴趣的片段需要多个步骤来引入药物中间体。拟议的项目将使用最近在Chao-Jun Li教授实验室发现的新颖烷基化反应来解决这个问题。该项目将寻求新的化学物质，使先进药物的功能化一步到位。该研究将集中在优化反应条件，使化学选择性和官能团耐受的转化成为可能。* 该项目的成功将是制药行业研究和开发的重大进步。