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- Title
Flow Synthesis of a Thiazolidine Drug Intermediate in Capillary Microreactors.
- Authors
de Oliveira Silva, Renan Rodrigues; Cuesta Calvo, Paulo Victor; Fernandes da Silva, Milena; Solisio, Carlo; Converti, Attilio; Alves Palma, Mauri Sergio
- Abstract
Microreactor technology can help to reduce the time to market new drugs. It was applied to produce (Z)‐5‐benzylidenethiazolidine‐2,4‐dione, a heterocyclic intermediate in the synthesis of various drugs. Ethanol was the optimum solvent and piperidine the best catalyst in the batch process. The continuous/microreactor process exhibited a much better performance than the batch process. The productivity, which was strongly influenced by solvent and temperature, reached a maximum at 160 °C using methanol as solvent. A kinetic/thermodynamic study indicated that the reaction followed the second‐order model and allowed estimating its main thermodynamic parameters. A product recovery protocol was finally proposed. The microreactor proved an efficient alternative to the batch reactor in scaling up the production of active pharmaceutical ingredients. Microreactor technology can reduce the time to place a new drug on the market as it does not necessitate the usual scale‐up step in batch processes. At proper temperatures, pressures, and average residence times, the productivity and yields of a continuous‐flow process in microreactors are higher than in the batch process. Consequently, the generation of waste is much smaller.
- Subjects
MICROREACTORS; THIAZOLIDINEDIONES; THERMODYNAMICS; PHYSICAL &; theoretical chemistry; DRUG synthesis
- Publication
Chemical Engineering & Technology, 2019, Vol 42, Issue 2, p465
- ISSN
0930-7516
- Publication type
Article
- DOI
10.1002/ceat.201800473