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1. Continuous Flow Synthesis of 16-Dehydropregnenolone Acetate, a Key Synthon for Natural Steroids and Drugs

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   25 Jun 2024 | Contributor(s):: Mancino, Valentina, Cerra, Bruno, Piccinno, Alessandro, Gioiello, Antimo

   A telescoped multistep process to provide the continuous delivery of 16-dehydropregnenolone acetate (16-DPA) from diosgenin is described. The method was evaluated through batch screenings that helped to identify critical bottlenecks and flowability, and the best conditions were optimized in flow...

2. Multistep continuous-flow synthesis of (R)- and (S)-rolipram using heterogeneous catalysts

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   10 May 2024 | Contributor(s):: Tsubogo, Tetsu, Oyamada, Hidekazu, Kobayashi, Shū

   Chemical manufacturing is conducted using either batch systems or continuous-flow systems. Flow systems have several advantages over batch systems, particularly in terms of productivity, heat and mixing efficiency, safety, and reproducibility. However, for over half a century, pharmaceutical...

3. Continuous-Flow Multistep Synthesis of Cinnarizine, Cyclizine, and a Buclizine Derivative from Bulk Alcohols

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   10 May 2024 | Contributor(s):: Borukhova, Svetlana, Noël, Timothy, Hessel, Volker

   Cinnarizine, cyclizine, buclizine, and meclizine belong to a family of antihistamines that resemble each other in terms of a 1-diphenylmethylpiperazine moiety. We present the development of a four-step continuous process to generate the final antihistamines from bulk alcohols as the starting...

4. From p-Xylene to Ibuprofen in Flow: Three-Step Synthesis by a Unified Sequence of Chemoselective C−H Metalations

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   10 May 2024 | Contributor(s):: Lee, Hyune-Jea, Kim, Dong-Pyo, Kim, Heejin

   Ibuprofen was prepared from an inactive and inexpensive p-xylene by three-step flow functionalizations through chemoselective metalations of benzyl positions in sequence using an in situ generated LICKOR-type superbase. The flow approach in the microreactor facilitated the comprehensive...

5. Heating under High-Frequency Inductive Conditions: Application to the Continuous Synthesis of the Neurolepticum Olanzapine (Zyprexa)

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   10 May 2024 | Contributor(s):: Hartwig, Jan, Ceylan, Sascha, Kupracz, Lukas, Coutable, Ludovic, Kirschning, Andreas

   Hot chemistry! High-frequency inductive heating and flow chemistry are an ideal match for high-temperature synthesis. This is demonstrated in the multistep flow synthesis of the neurolepticum olanzapine (Zyprexa) that included three reactions with inductive heating and two purification steps...

6. The route from problem to solution in multistep continuous flow synthesis of pharmaceutical compounds

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   09 Jun 2023 | Contributor(s):: Bana, P, Orkenyi, RLovei, K, Lako, A, Turos, GI, Eles, J, Faigl, F, Greiner, I

   Recent advances in the field of continuous flow chemistry allow the multistep preparation of complex molecules such as APIs (Active Pharmaceutical Ingredients) in a telescoped manner. Numerous examples of laboratory-scale applications are described, which are pointing towards novel manufacturing...