Continuous flow Buchwald–Hartwig amination of a pharmaceutical intermediate
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Peer-reviewed
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Abstract
A flow process for direct amination of a pharmaceutically relevant substrate using a Pd-NHC based catalyst was demonstrated in a lab-scale mini-plant and in a pilot-scale plant. The lab-scale mini-plant was used to determine catalyst stability under recycling conditions. Results in the mini-plant have shown the maximum space–time yield between the three types of reactor systems: a batch reactor, a mini-plant and a pilot plant. A comprehensive life-cycle assessment study of the synthesis of organometallic catalysts and their impact on the overall LCA of flow vs. batch syntheses was developed. Combined with a simplified economic analysis, the LCA study confirmed the benefits of switching to flow.
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Keywords
flow chemistry, Buchwald-Hartwig amination, N-heterocyclic carbenes, life cycle assessment
Journal Title
Reaction Chemistry & Engineering
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Journal ISSN
2058-9883
2058-9883
2058-9883
Volume Title
1
Publisher
Royal Society of Chemistry
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Sponsorship
European Commission (246461)
The research leading to these results has received funding from the European Research Council under the European Union's Seventh Framework Programme (EC FP7) Grant Agreement n. [NMP2-SL-2012-280827].