Issue 2, 2016

Continuous flow Buchwald–Hartwig amination of a pharmaceutical intermediate

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

Supplementary files

Article information

Article type
Paper
Submitted
04 10 2015
Accepted
09 11 2015
First published
23 11 2015
This article is Open Access
Creative Commons BY license

React. Chem. Eng., 2016,1, 229-238

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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