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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Flow Synthesis of a Thiazolidine Drug Intermediate in Capillary Microreactors

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Author(s):
de Oliveira Silva, Renan Rodrigues [1] ; Cuesta Calvo, Paulo Victor [1] ; da Silva, Milena Fernandes [2] ; Solisio, Carlo [3] ; Converti, Attilio [3] ; Alves Palma, Mauri Sergio [1]
Total Authors: 6
Affiliation:
[1] Univ Sao Paulo, Dept Biochem & Pharmaceut Technol, Ave Prof Lineu Prestes 580, Bloco 16, BR-05508000 Sao Paulo, SP - Brazil
[2] Univ Fed Pernambuco, Biosci Ctr, Ave Prof Moraes Rego 1235, Cidade Univ, BR-50670901 Recife, PE - Brazil
[3] Genoa Univ, Dept Civil Chem & Environm Engn, Pole Chem Engn, Via Opera Pia 15, I-16145 Genoa - Italy
Total Affiliations: 3
Document type: Journal article
Source: CHEMICAL ENGINEERING & TECHNOLOGY; v. 42, n. 2, p. 465-473, FEB 2019.
Web of Science Citations: 1
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 degrees 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. (AU)

FAPESP's process: 14/07757-2 - Micro-reactors in the synthesis of pharmaceuticals
Grantee:Mauri Sergio Alves Palma
Support type: Regular Research Grants