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Flow Chemistry on Multigram Scale: Continuous Synthesis of Boronic Acids within 1 s

Andreas Hafner, Mark Meisenbach and Joerg Sedelmeier*

*Novartis Campus, Novartis Pharma AG, 4002 Basel, Switzerland, Email: joerg.sedelmeiernovartis.com

A. Hafner, M. Meisenbach, J. Sedelmeier, Org. Lett., 2016, 18, 3630-3633.

DOI: 10.1021/acs.orglett.6b01681


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Abstract

A simple continuous flow setup for handling and performing of organolithium chemistry on the multigram scale enables the synthesis of various compounds following a reaction sequence of Hal/Li exchange and electrophilic quench. It was possible to synthesize building blocks within a 1 s total reaction time and with a remarkable throughput of 60 g / h.

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Key Words

arylboronic acids, flow chemistry


ID: J54-Y2016