The scarcity of complex intermediates in pharmaceutical research motivates the pursuit of reaction optimization protocols on sub-milligram scales. In this presentation, the development of an automated flow-based synthesis platform, designed from commercially available components, that integrates both rapid nanomole scale reaction screening and micromole scale synthesis into a single modular unit will be discussed. This system was validated by exploring a diverse range of reaction variables in a Suzuki-Miyaura coupling on nanomole scale at elevated temperatures, generating LC-MS data points for 5760 reactions at a rate of &gt;1500 reactions per 24 hours. Through multiple injections of the same segment, the system directly produced micromole quantities of desired material. The optimal conditions were also replicated in traditional flow and batch mode at 50 to 200 milligram scale to provide good to excellent yields. Further application and recent developments of this novel flow technology will be presented.<br/>

Platform for automated nanomole scale reaction screening and micromole scale synthesis in flow

2019 Spring National Meeting

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