Synthesis of a high specific activity methyl sulfone tritium isotopologue of fevipiprant (NVP-QAW039)
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Luu, Van Tong, Goujon, Jean-Yves, Meisterhans, Christian, 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 |
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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 |