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Continuous Flow as Enabling Technology: Synthesis of Heteroaromatic Sulfinates as Bench Stable Cross-Coupling Partners

Lima, Fabio and Andre, Jerome and Marziale, Alexander and Greb, Andreas and Glowienke, Susanne and Meisenbach, Mark and Schenkel, Berthold and Martin, Benjamin and Sedelmeier, Joerg Mathias (2020) Continuous Flow as Enabling Technology: Synthesis of Heteroaromatic Sulfinates as Bench Stable Cross-Coupling Partners. Organic Letters. ISSN 1523-70601523-7052

Abstract

An enabling continuous flow setup for handling of unstable organolithium intermediates and synthesis of heteroaryl sulfinates on multigram scale is described. The developed continuous flow process allows for the synthesis and simple isolation of heteroaryl sulfinates which otherwise are challenging to access in classical batch mode. The lithium sulfinate salts prepared by this method were shown to be efficient reaction partners in palladium catalyzed C(sp2)−C(sp2) cross-coupling to access medicinally relevant bis-heteroaryl motifs.

Item Type: Article
Date Deposited: 15 Aug 2020 00:45
Last Modified: 15 Aug 2020 00:45
URI: https://oak.novartis.com/id/eprint/42717

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