Medinical Chemistry Technologies, Abbott Laboratories, Global Pharmaceutical Research and Development, Abbott Park, IL 60064, USA.
Molecules. 2011 Nov 2;16(11):9161-77. doi: 10.3390/molecules16119161.
Flow chemistry has gained considerable recognition as a simple, efficient, and safe technology for the synthesis of many types of organic and inorganic molecules ranging in scope from large complex natural products to silicon nanoparticles. In this paper we describe a method that adapts flow chemistry to the synthesis of libraries of compounds using a fluorous immiscible solvent as a spacer between reactions. The methodology was validated in the synthesis of two small heterocycle containing libraries. The reactions were performed on a 0.2 mmol scale, enabling tens of milligrams of material to be generated in a single 200 mL reaction plug. The methodology allowed library synthesis in half the time of conventional microwave synthesis while maintaining similar yields. The ability to perform multiple, potentially unrelated reactions in a single run is ideal for making small quantities of many different compounds quickly and efficiently.
流动化学作为一种简单、高效、安全的技术，已在合成各种有机和无机分子方面得到了广泛的认可，范围从大型复杂天然产物到硅纳米粒子。本文中，我们描述了一种将流动化学应用于化合物库合成的方法，该方法使用不混溶的氟相溶剂作为反应之间的间隔物。该方法学在两个含有小杂环的化合物库的合成中得到了验证。反应在 0.2mmol 规模下进行，使得在单个 200mL 反应塞中能够生成数十毫克的产物。该方法在保持类似产率的同时，使库合成所需时间缩短了一半，与传统微波合成相当。在单个运行中进行多种潜在无关反应的能力非常适合快速有效地合成多种不同化合物的小批量。
