SBIR Phase I: 'Smart Filter' for Fast Chemical Reaction Clean-up

这个小型企业创新研究第一阶段项目名为？智能过滤器用于快速化学反应清理？解决了制造业中的一个重要问题，即化学合成的劳动密集型性质及其危险条件，不幸的是，在过去的60年里，这一问题没有太大变化。我们的新概念是？刚性溶剂萃取？通过消除液-液萃取步骤，加速反应清理。这个想法很简单：反应以通常的方式进行，用合适的水溶液淬灭；然而，我们不是使用相对大量的有机溶剂来提取水/有机混合物，而是使用固体支撑的有机液相(我们称之为？刚性溶剂?阶段)。？刚性溶剂?比液体更容易处理。我们的清洁墨盒设计也很简单，它是一个充满高多孔刚性有机聚合物的墨盒。反应清理墨盒解决了高通量合成部署与色谱柱分析进步之间存在的技术差距。由于化合物的合成和最终的纯化之间的后续步骤是费力的，我们的技术将大大缩小这一差距，提供一种有效和安全的处理潜在危险化学物质的替代方法。这个项目更广泛的影响/商业潜力在于它有可能在大多数化学制造过程的发现阶段降低成本和提高化学操作的安全性，包括药品、农用化学品或先进材料。大量化合物的制备量从毫克到克或公斤不等。在药物发现和临床前阶段，平均估计要测试10,000种化合物，才能研制出一种成功的药物。这数千种化合物的单独合成需要5到10个步骤，每个步骤都需要从商业上可用的原料中合成。需要合成的化合物的绝对数量构成了药物化学家的噩梦。反应清理的劳动密集型性质和不断上升的劳动力成本导致传统上在美国进行的合成化学工作外包给其他发展中国家，这些国家的劳动力更便宜，工人保护不那么严格，废物处理法规也不严格。我们公司？刚性解决方案，旨在开发一种自动化产品，可以减少合成化学的劳动密集型，并为工人提供更好的保护，免受有害物质的侵害，从而降低劳动力成本，合成时间和浪费，并帮助保持美国的化学合成工作。

This Small Business Innovation Research Phase I project entitled ?Smart Filter for Fast Chemical Reaction Clean-up? tackles an important problem in the manufacturing industry, namely, the labor-intensive nature of chemical synthesis and its hazardous conditions, which, unfortunately, have not changed much in the last 60 years. Our novel concept of ?rigid solvent extraction? speeds up reaction clean-up, by elimination of the liquid-liquid extraction step. The idea is very simple: reactions are conducted in the usual way and quenched with a suitable aqueous solution; however, instead of using relatively large amounts of organic solvent to extract the aqueous/organic mixture, we use a solid supported organic liquid phase (that we call a ?rigid solvent? phase). ?Rigid solvents? are easier to handle than liquids. Our clean-up cartridge design is also simple, it is a cartridge filled with highly porous rigid organic polymer. The reaction cleanup cartridges address the technology gap that exists between the deployment of high throughput synthesis and the analytical advances in chromatography columns. Because the workup step that lies between the synthesis of a compound and its final purification is laborious our technology will significantly close that gap providing an efficient and safe handling alternative of potentially hazardous chemistries. The broader impact/commercial potential of this project lies in its potential to reduce costs and improve safety in chemical operations during the discovery stage of most chemical manufacturing processes, including pharmaceuticals, agrochemicals, or advanced materials, a large number of compounds need to be prepared in amounts that range from mg to g or kg. An estimated 10,000 compounds are tested on average during drug discovery and preclinical stages in order to come up with one successful drug. And the individual synthesis of these thousands of compounds require between five to ten synthetic steps each from commercially available raw materials. The sheer number of compounds that need to be synthesized constitutes a nightmare scenario for medicinal chemists. The labor intensive nature of reaction clean-ups and rising labor costs have caused the outsourcing of synthetic chemistry work, traditionally conducted in the US, to other developing countries that have cheaper labor, less stringent worker protection, and lax waste disposal regulations. Our company ? Rigid Solutions, aims to develop an automation product that can make synthetic chemistry less labor-intensive and offer better protection for workers from hazardous substances, thereby reducing labor costs, synthesis time, and waste, and helping to keep chemical synthesis jobs in the US.