New strategies and methods in synthetic aromatic and heteroaromatic chemistry

合成芳烃和杂芳烃化学的新策略和新方法

• 批准号: 4538-2010
• 负责人: Snieckus, Victor
• 金额: $ 6.56万
• 依托单位: Queen's University
• 依托单位国家: 加拿大
• 项目类别: Discovery Grants Program - Individual
• 财政年份: 2014
• 资助国家: 加拿大
• 起止时间: 2014-01-01 至 2015-12-31
• 项目状态: 已结题
• 来源: https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=544200
• 关键词: New; strategies; methods; synthetic; aromatic

Synthetic chemists strive to build molecules, simple and complex, real and imaginary, which produce tomorrow's beneficial medicines and materials for humankind. They apply tested theories and new hypotheses to develop new types of starting materials and reagents, click them together in different ways like Lego blocks, and create a multitude of new products: a combination drug for AIDS, a derivative of taxol for breast cancer, a crucially needed anti-Alzheimer's drug, a smart material or a sensor. Our major themes concern the discovery and development of new synthetic methods for aromatics and heteroaromatics based on anionic and transition metal catalyzed reactions. We use directed ortho metalation (DoM) chemistry as a conceptual platform for invention of efficient synthetic methods, construction of bioactive and natural products and new chiral ligands, and for uncovering new links to emerging reactions in organic synthesis. MAJOR GOALS. We will pursue a number of recent discoveries in our labs to contribute to contemporary synthetic chemistry: a) reactions we have devised and developed (DoM-Suzuki) which are finding increased utility in academic and industrial laboratories, b) new reactions (e.g. catalytic C-O, C-N bond coupling processes, DoM-Petasis processes for bioactive benzylamines, unprecedented DoM-halogen rearrangements for biological pyridines, e.g. Vitamin B6) which we shall establish as robust methods for the same purpose, and c) application of discovered reactions to the total synthesis of biologically significant natural products. SYNTHETIC AROMATIC CHEMISTRY is a major component of the chemical enterprise today. Over 80% of current therapeutic agents contain aromatic or heteroaromatic moieties. Our reactions are being used by industry (e.g. Monsanto, Pfizer, BMS, Merck) for the multi-kg production of drugs, agrochemicals, and liquid crystals. IN OUR EFFORTS we aim to advance fundamental research, to heed the needs of medicinal and process chemists, and to train students for independent careers (68 MSc, PhD and postdoc students have been trained in the past 6 years).

合成化学家努力构建分子，简单的和复杂的，真实的和想象的，为人类生产明天有益的药物和材料。他们应用经过验证的理论和新的假设来开发新型的起始材料和试剂，像乐高积木一样以不同的方式将它们点击在一起，并创造出众多的新产品：艾滋病的组合药物，乳腺癌的紫杉醇衍生物，急需的抗阿尔茨海默病药物，智能材料或传感器。我们的主要主题是发现和开发基于阴离子和过渡金属催化反应的芳香族化合物和杂芳香族化合物的新合成方法。 我们使用定向邻位金属化（DoM）化学作为一个概念平台，用于发明有效的合成方法，构建生物活性和天然产物以及新的手性配体，并揭示有机合成中新兴反应的新联系。主要目标。我们将在我们的实验室中追求一些最新的发现，为当代合成化学做出贡献：a）我们设计和开发的反应（DoM-Suzuki），其在学术和工业实验室中的实用性增加，B）新反应（例如催化C-O、C-N键偶联方法，用于生物活性苄胺的DoM-Petasis方法，用于生物吡啶的前所未有的DoM-卤素重排，例如维生素B6），我们将建立用于相同目的的稳健方法，以及c）将所发现的反应应用于生物学上重要的天然产物的全合成。芳烃化工是当今化工企业的重要组成部分。超过80%的当前治疗剂含有芳族或杂芳族部分。我们的反应被工业界（如孟山都、辉瑞、BMS、默克）用于生产多公斤的药物、农用化学品和液晶。在我们的努力，我们的目标是推进基础研究，注意医药和过程化学家的需求，并培养学生独立的职业生涯（68硕士，博士和博士后学生已在过去6年中接受了培训）。