Methods for and Synthesis of Natural Product Hybrids for Medicinal Chemistry Applications

用于药物化学应用的天然产物杂化物的方法和合成

• 批准号: RGPIN-2014-06304
• 负责人: Dake, Gregory
• 金额: $ 2.48万
• 依托单位: University of British Columbia
• 依托单位国家: 加拿大
• 项目类别: Discovery Grants Program - Individual
• 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=648526
• 关键词: Methods; Synthesis; Natural; Product; Hybrids

This proposal deals with chemistry related to the science of synthetic organic chemistry. The science of organic chemistry is the science that examines the construction of organic (meaning built mostly of carbon, hydrogen, nitrogen and oxygen atoms) molecules. Similar to an architect designing a building, and engineers and construction workers building it based on that design, synthetic organic chemists design routes to, and build, organic molecules. Because of the complexity of organic molecules that Nature makes, synthetic organic chemists require new methods (the tools) to build these new molecules. Once these tools are designed, they are tested in the course of a complex molecule synthesis. **This research program embraces the development of new methodology that can be harnessed to produce compounds with a goal for increased understanding, or treatment, of human disease. Fundamental questions in catalysis include the study of catalyzed alkyne-diene Diels-Alder processes (Rh or Ni), interception of organometallic fragments using Csp nucleophiles (Pd), tandem activations of bisindoles (Rh) and tandem formations of bisindoles (Pd). Functional natural product like molecules (based on highly bioactive natural products) will be used to explore biological constructs related to human health, specifically malaria and cancer. **The described research will provide crucial advanced training for HQP interested in academic, industrial and biotechnology positions. HQP trained in these techniques traditionally end up working in fields related to the discovery of new medicines and new materials. Consequently, society receives many benefits through the efforts of HQP trained in the field of synthetic organic chemistry.

这一建议涉及与合成有机化学科学有关的化学。有机化学是一门研究有机分子（主要由碳、氢、氮和氧原子组成）结构的科学。类似于建筑师设计建筑物，工程师和建筑工人根据设计建造它，合成有机化学家设计路线并建造有机分子。由于大自然制造的有机分子的复杂性，合成有机化学家需要新的方法（工具）来构建这些新分子。一旦这些工具被设计出来，它们将在复杂分子合成过程中进行测试。** 该研究计划包括开发新的方法，可以利用这些方法来生产化合物，以提高对人类疾病的理解或治疗。催化的基本问题包括研究催化的炔-二烯Diels-Alder过程（Rh或Ni），使用Csp亲核试剂（Pd）拦截有机金属片段，双吲哚（Rh）的串联活化和双吲哚（Pd）的串联形成。功能性天然产物类分子（基于高生物活性天然产物）将用于探索与人类健康相关的生物结构，特别是疟疾和癌症。 ** 所述研究将为对学术，工业和生物技术职位感兴趣的HQP提供关键的高级培训。传统上，接受过这些技术培训的HQP最终会在与发现新药和新材料有关的领域工作。因此，通过在合成有机化学领域接受培训的HQP的努力，社会获得了许多好处。