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High-Throughput Platform for Novel Reaction Discovery
Authors:Xiao Lu  Zhiji Luo  Ruili Huang  Donald C Lo  Dr Wenwei Huang
Institution:1. Therapeutic Development Branch, National Center for Advancing Translational Sciences (NCATS), National Institutes of Health (NIH), Rockville, MD-20850 USA

These authors contributed equally to this work.;2. Chemical Genomics Branch, National Center for Advancing Translational Sciences (NCATS), National Institutes of Health (NIH), Rockville, MD-20850 USA;3. Therapeutic Development Branch, National Center for Advancing Translational Sciences (NCATS), National Institutes of Health (NIH), Rockville, MD-20850 USA

Abstract:Detecting the formation of new chemical bonds in high-throughput synthesis is limited by the efficiency and scalability of reaction product detection, as conventional methods for isolating product from reaction mixtures are time consuming and labor intensive. Here, we report a miniaturizable purification method that enables the rapid, high-throughput isolation of quaternary ammonium-tagged products from reaction mixtures with excellent purity using inexpensive equipment that easily can be set up in a typical organic chemistry laboratory. This novel purification technique enabled us to establish a high-throughput reaction discovery platform. We validated this platform in a screen of 1536 reactions, and one previously unreported transformation was identified.
Keywords:high-throughput screening  synthetic methods  UV/Vis spectroscopy
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