-
Continuous Flow Synthesis of 16-Dehydropregnenolone Acetate, a Key Synthon for Natural Steroids and Drugs
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...
-
Multistep continuous-flow synthesis of (R)- and (S)-rolipram using heterogeneous catalysts
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...
-
Continuous-Flow Multistep Synthesis of Cinnarizine, Cyclizine, and a Buclizine Derivative from Bulk Alcohols
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...
-
From p-Xylene to Ibuprofen in Flow: Three-Step Synthesis by a Unified Sequence of Chemoselective C−H Metalations
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...
-
Heating under High-Frequency Inductive Conditions: Application to the Continuous Synthesis of the Neurolepticum Olanzapine (Zyprexa)
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...
-
The route from problem to solution in multistep continuous flow synthesis of pharmaceutical compounds
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...