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首页> 外文期刊>Proceedings of the National Academy of Sciences of the United States of America >A general protocol for creating high-throughput screening assays for reaction yield and enantiomeric excess applied to hydrobenzoin
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A general protocol for creating high-throughput screening assays for reaction yield and enantiomeric excess applied to hydrobenzoin

机译：创建高通量筛选测定的一般方案，用于反应产率和对映体过量，适用于氢安息香

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摘要

A general approach to high-throughput screening of enantiomeric excess (ee) and concentration was developed by using indicator displacement assays (IDAs), and the protocol was then applied to the vicinal diol hydrobenzoin. The method involves the sequential utilization of what we define herein as screening, training, and analysis plates. Several enantioselective boronic acid-based receptors were screened by using 96-well plates, both for their ability to discriminate the enantiomers of hydrobenzoin and to find their optimal pairing with indicators resulting in the largest optical responses. The best receptor/indicator combination was then used to train an artificial neural network to determine concentration and ee. To prove the practicality of the developed protocol, analysis plates were created containing true unknown samples of hydrobenzoin generated by established Sharpless asymmetric dihydroxylation reactions, and the best ligand was correctly identified.
机译：通过使用指示剂置换试验（IDA），开发了一种高通量筛选对映体过量（ee）和浓度的通用方法，然后将该方案应用于邻二醇二氢苯偶姻。该方法涉及对本文定义的筛查，训练和分析板的顺序利用。通过使用96孔板筛选了几种基于对映选择性硼酸的受体，既具有区分氢安息香的对映异构体的能力，又具有与指示剂的最佳配对的能力，从而导致最大的光学响应。然后将最佳的受体/指标组合用于训练人工神经网络以确定浓度和ee。为了证明所开发方案的实用性，创建了分析板，其中包含由已建立的Sharpless不对称二羟基化反应生成的真正未知的氢安息香样品，并正确鉴定了最佳配体。

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