Miniaturized high-throughput chemistry technologies have time and again proven to be an efficient and effective technology to unearth new chemical methodologies, optimize reactions and provide compreshensive data sets to inform reaction predictive models. Exploitation of this technology to simultaneously study reaction optimization as a function of building-block and scaffold diversity has allowed us to rapidly access novel chemical entities while minimizing the risk of ‘failed’ reactions that often lead to desired compounds remaining unfurnished. Herein, we demonstrate that these micro-scale crude reactions can be utilized directly in a number of biological assay formats if appropriate experimental controls are added.  This combined process which we have termed ‘direct-to-biology’ (D2B), can significantly reduce medicinal chemistry program cycletimes by maximizing throughput, improving reaction success rates, and enhancing chemical space exploration while minimizing time consuming iterative single compound synthesis and purification. This work describes the development of an end-to-end nanoscale D2B workflow validated against two assay modalities: FLIPR and ASMS.

Development of a Nanoscale Chemistry Direct-to-Biology (D2B) Platform

ACS Spring 2022

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