Cross-Coupling Reactions Leading to Chiral Heterocyclic Scaffolds for Drug Development and Manufacturing

交叉偶联反应产生用于药物开发和制造的手性杂环支架

• 批准号: 536415-2018
• 负责人: OrellanaGarcia, JosueArturoJA
• 金额: $ 4.05万
• 依托单位: York University
• 依托单位国家: 加拿大
• 项目类别: Collaborative Research and Development Grants
• 财政年份: 2022
• 资助国家: 加拿大
• 起止时间: 2022-01-01 至 2023-12-31
• 项目状态: 已结题
• 来源: https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=747578
• 关键词: Cross; Coupling; Reactions; Leading; Chiral

Heterocycles, cyclic molecules with at least one non-carbon atom, are widely used in drug discovery and development due to their favourable physical and chemical properties. Pyridines are the most widely used aromatic heterocycle in FDA approved drugs and there is a continued demand for methods to prepare them and their derivatives. Unfortunately, the majority of methods to do this employ harsh reaction conditions and are therefore not widely useful. We have devised a conceptually new approach to make pyridine derivatives using exceptionally mild conditions that tolerate a wide range of functional groups. These reactions also provide immediate access to small molecules that possess 'drug-like' qualities and that are hard to make by other means. Finally, our methods are catalytic and therefore will contribute to the reduction of the environmental costs of drug discovery and development. As a result, the proposed research will have a direct impact on the search for new therapeutic agents.

杂环化合物是一种具有至少一个非碳原子的环状分子，由于其良好的物理和化学性质而广泛应用于药物发现和开发。吡啶是 FDA 批准的药物中使用最广泛的芳香杂环，并且对制备它们及其衍生物的方法有持续的需求。不幸的是，大多数方法都采用苛刻的反应条件，因此没有广泛使用。我们设计了一种概念上新的方法，使用能够耐受多种官能团的极其温和的条件来制造吡啶衍生物。这些反应还可以立即获得具有“类似药物”性质且难以通过其他方法制备的小分子。最后，我们的方法具有催化作用，因此将有助于降低药物发现和开发的环境成本。因此，拟议的研究将对寻找新的治疗药物产生直接影响。