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Transposition of a triphosgene-based process for pharmaceutical development: from mg·h-1 to kg·h-1 of an unsymmetrical urea

Leroyer, Léo and Prat, Laurent E. and Cabassud, Michel and Gourdon, Christophe and Dechy-Cabaret, Odile and Barthes, Matthieu and Camus, Philippe and Hattou, Stephane Transposition of a triphosgene-based process for pharmaceutical development: from mg·h-1 to kg·h-1 of an unsymmetrical urea. (2013) Green Processing and Synthesis, 2 (3). 1-12. ISSN 2191-9542

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Official URL: https://doi.org/10.1515/gps-2013-0026

Abstract

A two reaction synthesis of a urea, using triphosgene, was studied. The objective was to transpose the process from laboratory scale to pre-industrial plant. The whole study was performed in a continuous process, adapting the characteristic dimensions and length of the reactor. In this paper, the development of the process is presented, and the choices about safety and operating conditions constraints are discussed. The final operation allows a 70% global yield in a 7 week study. Furthermore, the use of microreactors not only permits an exhaustive study of the process operating parameters, but also provides feedback on the developed chemistry itself. The results obtained are a demonstration of the use of continuous processes in small scale reactors for complex molecule development. The mg·h-1 to kg·h-1 is a key transposition in the pharmaceutical industries project development, as it can help to accelerate the first lot production used in toxicological or pre-clinic stages.

Item Type:Article
Additional Information:Open access - Attribution-NonCommercial-NoDerivs 3.0 Unported (CC BY-NC-ND 3.0)
Audience (journal):International peer-reviewed journal
Uncontrolled Keywords:
Institution:French research institutions > Centre National de la Recherche Scientifique - CNRS (FRANCE)
Université de Toulouse > Institut National Polytechnique de Toulouse - Toulouse INP (FRANCE)
Other partners > Sanofi Aventis (FRANCE)
Université de Toulouse > Université Toulouse III - Paul Sabatier - UT3 (FRANCE)
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Deposited On:16 Feb 2021 16:06

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