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Synthesis of a high specific activity methyl sulfone tritium isotopologue of fevipiprant (NVP-QAW039)

Luu, Van Tong and Goujon, Jean-Yves and Meisterhans, Christian and Frommherz, Matthias and Bauer, Carsten (2014) Synthesis of a high specific activity methyl sulfone tritium isotopologue of fevipiprant (NVP-QAW039). Journal of Radiolabelled Compounds and Radiopharmaceuticals.

Abstract

The synthesis of a triple tritiated isotopologue of the CRTH2 antagonist NVP-QAW039 (fevipiprant) with a specific activity > 3TBq/mmol is described. Key to the high specific activity is the use of a bench stable dimeric precursor which is reduced to the monomer and methylated with [3H3]MeONos using techniques usually known in chemical cross-linking of biomacromolecules.

Item Type: Article
Keywords: Tritium - CRTH2 receptor antagonists – NVP-QAV680 - NVP-QAW039 - fevipiprant - 3-(2-methyl-7-aza-indolyl) acetic acid - chemical cross-linking – [3H3]methyl nosylate - Palladium catalysis
Date Deposited: 13 Oct 2015 13:12
Last Modified: 13 Oct 2015 13:12
URI: https://oak.novartis.com/id/eprint/23026

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