Continuous slurry plug flow Fe/ppm Pd nanoparticle-catalyzed Suzuki–Miyaura couplings in water utilizing novel solid handling equipment

• Alex B. Wood^a
• Scott Plummer^b
• Richard I. Robinson^b
• Marie Smith^c
• Jim Chang^c
• Fabrice Gallou^d
• Bruce H. Lipshutz^a

• ^aDepartment of Chemistry and Biochemistry, University of California, Santa Barbara, CA 93106, USA
• ^bGlobal Discovery Chemistry – Chemistry Technology Group, Novartis Institutes for Biomedical Research, 250 Massachusetts Avenue, Cambridge, MA 02139, USA
• ^cGenomics Institute of the Novartis Research Foundation, 10675 John J Hopkins Dr., San Diego, CA 92121, USA
• ^dNovartis Pharma AH, CH-4057 Basel, Switzerland

Herein are reported initial efforts to develop a generally accessible flow process, applying a heterogenous nanocatalyst to aqueous micelle-enabled Suzuki–Miyaura coupling reactions. Also disclosed is a new engineering solution (i.e., a self-draining back pressure regulator), which, when applied, enabled 1.5 hours of continuous operation leading to the production of 20 grams of a pharmaceutical intermediate.

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