Chemical space is vast, and chemical reactions involve the complex interplay of multiple variables. As a consequence, reactions can fail for subtle reasons, necessitating screening of conditions. High-throughput experimentation (HTE) techniques enable a more comprehensive array of data to be obtained in a relatively short amount of time. Although HTE can be most efficiently achieved with automated robotic dispensing equipment, the benefits of running reaction microarrays can be accessed in any regularly equipped laboratory using inexpensive consumables. Herein, we present a cost-efficient approach to HTE, examining a Buchwald–Hartwig amination as our model reaction. Experiments are carried out in a machined aluminum 96-well plate, taking advantage of solid transfer scoops and pipettes to facilitate rapid reagent transfer. Reaction vials are simultaneously heated and mixed, using a magnetic stirrer, and worked up in parallel, using a plastic filter plate. Analysis by gas chromatography provides the chemist with 96 data points with minimal commitment of time and resources. The best-performing experiment can be selected for scale-up and isolation, or the data can be used for designing future optimization experiments.

化学空间广阔，化学反应涉及多个变量的复杂相互作用。因此，反应可能因微妙的原因而失败，因此需要筛选条件。高通量实验 (HTE) 技术可以在相对较短的时间内获得更全面的数据阵列。虽然 HTE 可以通过自动机器人分配设备最有效地实现，但运行反应微阵列的好处可以在任何使用廉价耗材的定期配备的实验室中获得。在此，我们提出了一种具有成本效益的 HTE 方法，将 Buchwald-Hartwig 胺化作为我们的模型反应。实验在机加工的铝制 96 孔板中进行，利用固体转移勺和移液器促进快速试剂转移。使用磁力搅拌器同时加热和混合反应瓶，并使用塑料滤板平行处理。气相色谱法分析为化学家提供了 96 个数据点，而投入的时间和资源最少。可以选择表现最佳的实验进行放大和分离，或者数据可用于设计未来的优化实验。