A small footprint oxycodone generator based on continuous flow technology and real-time analytics
- Florian Sommera,b
- David Cantilloa,b
- C. Oliver Kappea,b
- aInstitute of Chemistry, University of Graz, NAWI Graz, Heinrichstrasse 28, 8010, Graz, Austria
- bCenter for Continuous Flow Synthesis and Processing (CCFLOW), Research Center Pharmaceutical Engineering GmbH (RCPE), Inffeldgasse 13, 8010, Graz, Austria
Read the publication that featured this abstractA scalable continuous flow setup for the preparation of the opioid medication oxycodone is presented. The process is based on a two-step synthetic sequence consisting of C14 hydroxylation of thebaine with performic acid, followed by catalytic hydrogenation of the ensuing 14-hydroxycodeinone intermediate. Safe and efficient oxidation with performic acid has been achieved by generating the reagent in situ in the presence of the starting material using a micromixer. Catalytic hydrogenation has been carried out in a scalable shell-and-tube reactor equipped with palladium-electroplated catalytic static mixers. Acquisition of real-time process data has been enabled by integrating online UHPLC analysis at the reactor output. The continuous process features safe operation, high atom economy, simple workup and production of 7 g/h of high purity oxycodone in a small footprint setup.
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