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Open AccessArticle

Enantioselective Organocatalysis in Microreactors: Continuous Flow Synthesis of a (S)-Pregabalin Precursor and (S)-Warfarin

Dipartimento di Chimica, Università degli Studi di Milano, Via Golgi 19, Milano I-20133, Italy
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Academic Editor: Svetlana Tsogoeva
Symmetry 2015, 7(3), 1395-1409; https://doi.org/10.3390/sym7031395
Received: 10 June 2015 / Revised: 26 June 2015 / Accepted: 17 July 2015 / Published: 4 August 2015
(This article belongs to the Special Issue Asymmetric Catalysis)
Continuous flow processes have recently emerged as a powerful technology for performing chemical transformations since they ensure some advantages over traditional batch procedures. In this work, the use of commercially available and affordable PEEK (Polyetheretherketone) and PTFE (Polytetrafluoroethylene) HPLC (High Performance Liquid Chromatography) tubing as microreactors was exploited to perform organic reactions under continuous flow conditions, as an alternative to the commercial traditional glass microreactors. The wide availability of tubing with different sizes allowed quickly running small-scale preliminary screenings, in order to optimize the reaction parameters, and then to realize under the best experimental conditions a reaction scale up for preparative purposes. The gram production of some Active Pharmaceutical Ingredients (APIs) such as (S)-Pregabalin and (S)-Warfarin was accomplished in short reaction time with high enantioselectivity, in an experimentally very simple procedure. View Full-Text
Keywords: asymmetric synthesis; organocatalysis; flow chemistry; microreactors; active pharmaceutical ingredients; PEEK tubing asymmetric synthesis; organocatalysis; flow chemistry; microreactors; active pharmaceutical ingredients; PEEK tubing
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Porta, R.; Benaglia, M.; Coccia, F.; Rossi, S.; Puglisi, A. Enantioselective Organocatalysis in Microreactors: Continuous Flow Synthesis of a (S)-Pregabalin Precursor and (S)-Warfarin. Symmetry 2015, 7, 1395-1409.

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