Kilogram-Scale Synthesis of the CXCR4 Antagonist GSK812397

An improved, scalable synthesis of the CXCR4 antagonist GSK812397 is described. This new route was recently scaled up in 50 L fixed equipment to afford 1.2 kg of drug substance in five steps with an overall yield of 20% and >99% chemical and enantiomeric purity.

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Published in:Organic process research & development 2009-07, Vol.13 (4), p.781-785
Main Authors: Boggs, Sharon, Elitzin, Vassil I, Gudmundsson, Kristjan, Martin, Michael T, Sharp, Matthew J
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Language:English
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container_title Organic process research & development
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creator Boggs, Sharon
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description An improved, scalable synthesis of the CXCR4 antagonist GSK812397 is described. This new route was recently scaled up in 50 L fixed equipment to afford 1.2 kg of drug substance in five steps with an overall yield of 20% and >99% chemical and enantiomeric purity.
doi_str_mv 10.1021/op9000675
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source American Chemical Society:Jisc Collections:American Chemical Society Read & Publish Agreement 2022-2024 (Reading list)
title Kilogram-Scale Synthesis of the CXCR4 Antagonist GSK812397
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