Removal of Alkyl Sulfonates Using DABCO

During the route development of a midstage clinical candidate, we were challenged with a presence of alkyl sulfonates, which were identified as potential genotoxic impurities in our active pharmaceutical ingredient (API). As a result, we initiated a development effort to identify a method to remove...

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Veröffentlicht in:Organic process research & development 2022-03, Vol.26 (3), p.987-993
Hauptverfasser: Corazzata, Kaitlyn, Rose, Peter J, Mo, Shunyan, Snodgrass, Joseph, Langston, Alexander, Lee, Elaine C
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container_issue 3
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container_title Organic process research & development
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creator Corazzata, Kaitlyn
Rose, Peter J
Mo, Shunyan
Snodgrass, Joseph
Langston, Alexander
Lee, Elaine C
description During the route development of a midstage clinical candidate, we were challenged with a presence of alkyl sulfonates, which were identified as potential genotoxic impurities in our active pharmaceutical ingredient (API). As a result, we initiated a development effort to identify a method to remove the alkyl sulfonates that would be amenable for scale-up. Herein, we report our effort toward the development of a general approach using DABCO (1,4-diazabicyclo[2.2.2]­octane) to remove alkyl sulfonates that is both efficient and convenient from the bench to scale-up.
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