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Issue 2, 2016
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Continuous flow Buchwald–Hartwig amination of a pharmaceutical intermediate

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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.

Graphical abstract: Continuous flow Buchwald–Hartwig amination of a pharmaceutical intermediate

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Publication details

The article was received on 04 Oct 2015, accepted on 09 Nov 2015 and first published on 23 Nov 2015


Article type: Paper
DOI: 10.1039/C5RE00048C
Citation: React. Chem. Eng., 2016,1, 229-238
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    Continuous flow Buchwald–Hartwig amination of a pharmaceutical intermediate

    P. Yaseneva, P. Hodgson, J. Zakrzewski, S. Falß, R. E. Meadows and A. A. Lapkin, React. Chem. Eng., 2016, 1, 229
    DOI: 10.1039/C5RE00048C

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