Continuous flow Buchwald–Hartwig amination of a pharmaceutical intermediate. Issue 2 (23rd November 2015)

• Record Type: Journal Article
• Authors: Yaseneva, Polina; Hodgson, Paul; Zakrzewski, Jacek; Falß, Sebastian; Meadows, Rebecca E.; Lapkin, Alexei A.
• Is Part Of: Reaction chemistry & engineering. Volume 1:Issue 2(2016)
• Page Start: 229
• Page End: 238
• Publication Date: 2015-11-23
• Subjects: Reaction mechanisms (Chemistry) -- Periodicals; Chemical engineering -- Periodicals; Chemical engineering; Reaction mechanisms (Chemistry); Periodicals; 547.705
• DOI: 10.1039/c5re00048c
• Languages: English
• ISSNs: 2058-9883

Abstract

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. 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.