New Synthetic Strategies & Methods for Bioactive Aromatics and Heteroaromatics

新的合成策略

• 批准号: RGPIN-2015-05698
• 负责人: Snieckus, Victor
• 金额: $ 5.39万
• 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: 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=613697
• 关键词: New; Synthetic; Strategies; Methods; Bioactive

Importance of Organic Synthesis. Today, driving most advances in biology and material science is the science and art of making molecules – chemical synthesis. It allows for the practical supply of medicinals and materials that are difficult or impossible to acquire otherwise; it has profound consequences on human health (most therapeutic agents are synthesis-derived) and our standards of living (nanotubes, conducting polymers, smart phones, sensors). Fundamental discoveries in synthesis are at the heart of practical impact decades later, e.g. the 2010 Nobel and the 2014 Nobel (awarded for optical microscopy “allowing us to peer into the nanoworld” and track e.g. Alzheimer disease), is based on organic synthesis. The understanding of relationship of RNA and DNA is dependent on questions such as “why pentose and not hexose nucleic acids?” asked by organic chemists which will allow understanding of how life began (our prebiotic origins). Such basic questions must be answered before application in society, usually 20 years hence, can result. Our Research. We aim to discover methods for making molecules. Our focus is aromatic/heteroaromatic molecules since they make up 80% of current commercial drugs. Our major achievements are in the area of lithium organometallic chemistry and we have coupled these with modern catalytic transition metal chemistry. Our Impact. Aside from use on small scale in university labs, our fundamental research is now adapted worldwide in technologies for making marketable medicines and food protection agents, e.g. Sustiva™ (BMS, anti-AIDS), Silthiofam™ (Monsanto, fungicide), Losartan™ (BMS, anti-inflammatory), and very recently, a molecule (Merck) to inhibit an enzyme involved in pathological conditions, eg. anorexia, atherosclerosis, stroke. Our Future Goals. To continue in invention and enhancement of our focal themes of lithium and transition metal catalyzed reactions as platforms for new ways to make molecules which overcome today’s critical problems of the traditional lengthy, uneconomical, and environmentally unacceptable routes of the past. (Imagine a chemical reaction at Resolute Bay temperatures; we do that and, remarkably, industry can use our -78 0C reaction but now we have discovered how to use much more reasonable temperatures.) In context of our areas of expertise, we will develop new technology, e.g. flow microreactor, to encourage the use of our basic research in pharma and biotech to make the medicinal agents for human health for the future.

有机合成的重要性。今天，推动生物学和材料科学进步的是制造分子的科学和艺术-化学合成。它允许实际供应的药物和材料，是很难或不可能获得，否则;它对人类健康有深远的影响（大多数治疗剂是合成衍生）和我们的生活标准（纳米管，导电聚合物，智能手机，传感器）。合成的基本发现是几十年后实际影响的核心，例如2010年诺贝尔奖和2014年诺贝尔奖（授予光学显微镜“让我们窥视世界”并跟踪阿尔茨海默病）是基于有机合成。对RNA和DNA关系的理解依赖于诸如“为什么是戊糖而不是己糖核酸”之类的问题。有机化学家提出的问题，这将有助于了解生命是如何开始的（我们的生命起源）。这些基本问题必须在社会应用之前得到回答，通常是20年之后。 我们的研究。我们的目标是发现制造分子的方法。我们的重点是芳香族/杂芳香族分子，因为它们占当前商业药物的80%。我们的主要成就是在锂有机金属化学领域，我们已经将这些与现代催化过渡金属化学相结合。 我们的影响。除了在大学实验室中小规模使用外，我们的基础研究现在在全球范围内适用于制造可销售药物和食品保护剂的技术，例如Sustiva™（BMS，抗艾滋病），Silthiofam™（孟山都，杀真菌剂），Losartan™（BMS，抗炎），以及最近的分子（默克），以抑制参与病理条件的酶，例如。厌食动脉粥样硬化中风 我们的未来目标。继续发明和加强我们的锂和过渡金属催化反应的重点主题，作为新方法的平台，以克服当今传统的冗长，不经济和环境不可接受的过去路线的关键问题。（想象一下在Resolute Bay温度下的化学反应;我们这样做，值得注意的是，工业可以使用我们的-78 ℃反应，但现在我们已经发现如何使用更合理的温度。在我们的专业领域内，我们将开发新技术，例如流动微反应器，以鼓励利用我们在制药和生物技术方面的基础研究，为未来的人类健康制造药剂。