2018Chemical Engineering & TechnologyRequires access

Microreactor Technology as a Tool for the Synthesis of a Glitazone Drug Intermediate

Danilo da Silva Pinheiro, Renan Rodrigues de Oliveira Silva, Paulo Victor Cuesta Calvo, Milena Fernandes da Silva, Attílio Converti, Mauri Sérgio Alves Palma

Open publisher page 30 citations

Abstract

Abstract One of the bottlenecks in the pharmaceutical industry is drug production scale‐up, which can be performed by microreactor technology. Such an approach was applied to the synthesis of ( Z )‐5‐(4‐hydroxybenzylidene)thiazolidine‐2,4‐dione, a bioactive aromatic heterocyclic compound belonging to the class of glitazones. n ‐Propanol was the best solvent and piperidine the best catalyst for the batch reaction, which was completed in only 5.5 h. In the microreactor, the productivity was almost independent of solvent. The microreactor behaved as a plug‐flow reactor and operated at a steady state for ten hours without efficiency loss. The results suggest that microreactors may replace batch reactors in scaling up drug production.

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What this paper is about

Abstract One of the bottlenecks in the pharmaceutical industry is drug production scale‐up, which can be performed by microreactor technology. Such an approach was applied to the synthesis of ( Z )‐5‐(4‐hydroxybenzylidene)thiazolidine‐2,4‐dione, a bioactive aromatic heterocyclic compound belonging to the class of glitazones. n ‐Propanol was the best solvent and piperidine the best catalyst for the batch reaction, which was completed in only 5.5 h. In the microreactor, the productivity was almost independent of solvent. The microreactor behaved as a plug‐flow reactor and operated at a steady state for ten hours without efficiency loss. The results suggest that microreactors may replace batch reactors in scaling up drug production.

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Available abstract

Abstract One of the bottlenecks in the pharmaceutical industry is drug production scale‐up, which can be performed by microreactor technology. Such an approach was applied to the synthesis of ( Z )‐5‐(4‐hydroxybenzylidene)thiazolidine‐2,4‐dione, a bioactive aromatic heterocyclic compound belonging to the class of glitazones. n ‐Propanol was the best solvent and piperidine the best catalyst for the batch reaction, which was completed in only 5.5 h. In the microreactor, the productivity was almost independent of solvent. The microreactor behaved as a plug‐flow reactor and operated at a steady state for ten hours without efficiency loss. The results suggest that microreactors may replace batch reactors in scaling up drug production.

Key concepts: Microreactor, Flow chemistry, Chemistry, Solvent, Piperidine, Catalysis, Combinatorial chemistry, Batch reactor

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