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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Bibliographic Details
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
Format: Article
Language:English
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Description
Summary: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.
ISSN:1083-6160
1520-586X
DOI:10.1021/op9000675