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: 2010
• 资助国家: 加拿大
• 起止时间: 2010-01-01 至 2011-12-31
• 项目状态: 已结题
• 来源: https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=449693
• 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。他们运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，像乐高积木一样将它们以不同的方式组合在一起，创造出大量的新产品：治疗艾滋病的联合药物、治疗乳腺癌的紫杉醇衍生物、急需的抗阿尔茨海默氏症药物、智能材料或传感器。我们的主要课题是发现和发展基于阴离子和过渡金属催化反应的芳烃和杂芳烃的新合成方法。我们利用定向邻位金属化（DoM）化学作为一个概念平台，发明高效的合成方法，构建生物活性和天然产物以及新的手性配体，并发现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继续研究一些最近的发现，为当代合成化学做出贡献：a)我们设计和开发的反应（DoM-Suzuki）在学术和工业实验室中越来越实用，b)新的反应（例如催化C-O， C-N键偶联过程，生物活性苯胺的DoM-Petasis过程，生物吡啶的前所未有的dom -卤素重排，例如维生素B6），我们将建立同样目的的稳健方法。c)将发现的反应应用于具有重要生物学意义的天然产物的全合成。合成芳香族化学是当今化工企业的重要组成部分。目前超过80%的治疗剂含有芳香或杂芳香部分。我们的反应被工业（如孟山都、辉瑞、BMS、默克）用于多公斤级药物、农用化学品和液晶的生产。在我们的努力中，我们的目标是推进基础研究，关注药物和工艺化学家的需求，并培养学生独立的职业生涯（在过去的6年里，我们培养了68名硕士、博士和博士后学生）。