Synthesis of a diversified boron reagent library for drug development

用于药物开发的多样化硼试剂库的合成

• 批准号: 520481-2017
• 负责人: Legault, Claude
• 金额: $ 1.82万
• 依托单位: Université de Sherbrooke
• 依托单位国家: 加拿大
• 项目类别: Engage Grants Program
• 财政年份: 2017
• 资助国家: 加拿大
• 起止时间: 2017-01-01 至 2018-12-31
• 项目状态: 已结题
• 来源: https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=639648
• 关键词: Synthesis; diversified; boron; reagent; library

The health sector is facing numerous challenges. For example, the emergence of multidrug-resistant pathogensrequires the development of new antibiotic drugs to protect the population. In this context, organic synthesisplays a vital role. Indeed, the development of new synthetic methods and reagents for the creation andevaluation of new molecules of biological interest is the foundation on which we improve the drugs availableto treat illnesses. Consequently, there is a need to expand the pool of reagents available supporting drugdevelopment. One strategy is to use libraries of high-value building blocks reagents that enable rapid creationof complex and diverse molecules.Intellisyn is thus looking to acquire a diversified collection of highly-functionalized organotrifluoroborate saltsand boronic acids, which will greatly expand their reagents library. The goal of this project is to create suchlibrary, using reagents recently developed in our group. This will greatly expand the reagents library ofIntellisyn. The compounds furnished through this project are not available commercially and will greatlyfacilitate their drug development pipeline. It will consequently contribute to their competitiveness andexpansion in Canada. In addition, this project will enable the development of new arylation methods that willbe useful in the field of organic synthesis.

卫生部门面临着许多挑战。例如，多重耐药病原体的出现需要开发新的抗生素药物来保护人口。在这方面，有机合成起着至关重要的作用。事实上，开发新的合成方法和试剂来创造和评估具有生物学意义的新分子，是我们改进治疗疾病的药物的基础。因此，有必要扩大可用于支持药物开发的试剂库。其中一个策略是使用高价值的构建模块试剂库，以快速创建复杂和多样化的分子。因此，Intellisyn正在寻求获得高度官能化的有机三氟硼酸盐和硼酸的多样化集合，这将大大扩展他们的试剂库。这个项目的目标是创建这样的库，使用我们组最近开发的试剂。这将极大地扩展Intellisyn的试剂库。通过该项目提供的化合物没有商业化，将极大地促进其药物开发管道。因此，这将有助于他们在加拿大的竞争力和扩张。此外，该项目将使新的芳基化方法的发展，将在有机合成领域的有用。