Synthesis of Novel Indole-Based Heterocycles

新型吲哚基杂环化合物的合成

• 批准号: RGPIN-2015-05365
• 负责人: Jha, Mukund
• 金额: $ 1.46万
• 依托单位: Nipissing University
• 依托单位国家: 加拿大
• 项目类别: Discovery Grants Program - Individual
• 财政年份: 2016
• 资助国家: 加拿大
• 起止时间: 2016-01-01 至 2017-12-31
• 项目状态: 已结题
• 来源: https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=613506
• 关键词: Synthesis; Novel; Indole; Based; Heterocycles

Creative organic synthesis is a cornerstone for feeding the demands of numerous research areas (such as pharmaceuticals, agrochemicals, material sciences, catalysis, photochemistry, fragrances and pigments) where novel molecular frameworks with interesting properties and topology are constantly sought. It is crucial for synthetic chemists to develop and fine-tune reaction methodologies that enable efficient and green synthesis of the desired skeletons. The indole core is a prevalent substructure in many natural products and biologically active compounds. Due to its biological importance, indole based compounds attract special attention as a building block for the development of therapeutic agents by medicinal chemists. A plethora of bioactivities surrounding the indole-core continue to be a driving force in the development of new methodology to find useful compounds and increase the heterocyle diversity. Thus, the need for development of efficient and practical syntheses of indoles bearing a variety of substitution patterns is of great significance. The objective of my research program is to explore and develop novel and efficient synthetic methodology of indole heterocycles bearing a variety of substitution patterns. The long-term goal is to use the developed methodology to enrich the heterocycle diversity around indole nucleus to find commercially useful chemicals. The proposed research program will lead to novel indole-based molecular architectures with interesting biological properties and 3-D topology. These molecules could also serve as building blocks for synthesizing compounds of desired frameworks. Particular attention will be given to incorporating green properties (such as, clean and quantitative conversion, mild conditions, catalyst recycling, atom economy, one-pot cascade reactions, and low waste production) to methodologies developed in my laboratory in order to advance their practical and commercial importance. Approximately 25-30 students (HQP) will be trained over the tenure of the grant. The training received by HQPs will better prepare them to contribute to research activities in industry, government, and university laboratories across Canada.

创造性的有机合成是一个基石， 许多研究领域的需求（如制药，农用化学品， 材料科学、催化、光化学、香料和颜料）， 具有有趣性质和拓扑结构的新型分子框架， 不断追求。对于合成化学家来说， 微调反应方法，实现高效且绿色的合成 想要的骷髅吲哚核心是许多植物中普遍存在的亚结构 天然产物和生物活性化合物。由于其生物 重要的是，吲哚基化合物作为建筑物吸引了特别的注意， 药物化学家开发治疗剂的障碍。一 围绕吲哚核心的过多生物活性继续是一种驱动力， 开发新方法以寻找有用的化合物的力量， 增加杂环多样性。因此，需要开发高效的 以及具有多种取代模式的吲哚的实用合成 意义重大。我的研究项目的目标是探索 发展了吲哚杂环化合物的新型高效合成方法 带有多种替代模式。长期目标是使用 开发了丰富吲哚核周围杂环多样性的方法 来寻找商业上有用的化学品。 拟议的研究计划将导致新的吲哚基 具有有趣的生物学特性和3D的分子结构 topology.这些分子也可以作为合成 所需骨架的化合物。将特别注意 结合绿色特性（例如，清洁和定量转化， 温和条件，催化剂循环，原子经济性，一锅级联反应， 和低废物生产）的方法，在我的实验室， 以提高其实用性和商业重要性。大约25-30名学生（HQP）将在赠款的任期内接受培训。HQP接受的培训将使他们更好地为加拿大各地的工业，政府和大学实验室的研究活动做出贡献。