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1. Development of a Commercial Flow Barbier Process for a Pharmaceutical Intermediate

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   25 Jun 2024 | Contributor(s):: Braden, Timothy M., Johnson, Martin D., Kopach, Michael E., Groh, Jennifer McClary, Spencer, Richard D., Lewis, Jeffrey, Heller, Michael R., Schafer, John P., Adler, Jonathan J.

   A flow Barbier process was developed to produce a key intermediate in the edivoxetine·HCl registered sequence. The control strategy was developed based on a critical understanding of integrated parameters and design space requirements for a continuous stirred tank reactor (CSTR) process. In this...

2. Flow-oriented synthetic design in the continuous preparation of the aryl piperazine drug flibanserin

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   10 May 2024 | Contributor(s):: Bana, Péter, Szigetvári, Áron, Kóti, János, Éles, János, Greiner, István

   An uninterrupted, four-step continuous-flow sequence was developed for the preparation of the aryl piperazine-type serotonin receptor modulator drug, flibanserin. The unprecedented route was designed for efficient operation in flow, consisting of heterogeneously catalyzed reductive amination...

3. A Three-Minute Synthesis and Purification of Ibuprofen: Pushing the Limits of Continuous-Flow Processing

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   10 May 2024 | Contributor(s):: Snead, David R., Jamison, Timothy F.

   In a total residence time of three minutes, ibuprofen was assembled from its elementary building blocks with an average yield of above 90 % for each step. A scale-up of this five-stage process (3 bond-forming steps, one work-up, and one in-line liquid–liquid separation) provided ibuprofen at a...

4. Chemoenzymatic Synthesis in Flow Reactors: A Rapid and Convenient Preparation of Captopril

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   10 May 2024 | Contributor(s):: De Vitis, Valerio, Dall'Oglio, Federica, Pinto, Andrea, De Micheli, Carlo, Molinari, Francesco, Conti, Paola, Romano, Diego, Tamborini, Lucia

   The chemoenzymatic flow synthesis of enantiomerically pure captopril, a widely used antihypertensive drug, is accomplished starting from simple, inexpensive, and readily available reagents. The first step is a heterogeneous biocatalyzed regio- and stereoselective oxidation of cheap prochiral...