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Imaging agent of a TRPA1 inhibitor

Jonas Malmquist¹, Alexandra Bernlind, Sandra Lindberg

¹Isotope Chemistry, Screening and Profiling Global DMPK IM, AstraZeneca, Research & Development | Innovative Medicines, SE- 151 85, Södertälje, Sweden; Current address: Novandi Chemistry AB, Biovation Park Telge, SE- 151 85, Södertälje, Sweden.

Journal of Labelled Compounds & Radiopharmaceuticals

|November 29, 2013

Abstract:

A method for the preparation of [3'-(3) H]-4-(2'-chloro-6'-hydroxyphenyl)-2-thioxo-3,4-dihydro-1H-indeno[1,2-d]pyrimidin-5(2H)-one (1), a TRPA1 inhibitor, was developed for the evaluation of imaging properties of a class of TRPA1 inhibitors. 1 was prepared via tritiation of a protected benzaldehyde followed by a tetrachlorosilane catalyzed multicomponent one-step fusion and was obtained at a specific activity of 0.9 TBq/mmol. A (3) H-NMR spectrum on 13.5 MBq at 75 μM was recorded.

Keywords:

3H NMR TRPA1 isotopically labeled synthesis

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