Imaging agent of a TRPA1 inhibitor.

J Labelled Comp Radiopharm

Isotope 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.

Published: August 2014

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.

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http://dx.doi.org/10.1002/jlcr.3030DOI Listing

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