title: Imaging agent of a TRPA1 inhibitor.
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.
authors.affiliation: 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.
authors.forename: Jonas
authors.initials: J
authors.lastname: Malmquist
authors.forename: Alexandra
authors.initials: A
authors.lastname: Bernlind
authors.forename: Sandra
authors.initials: S
authors.lastname: Lindberg
mesh_terms: D007192:Indenes / Q000737:chemistry* / Q000494:pharmacology*; D011743:Pyrimidines / Q000737:chemistry* / Q000494:pharmacology*; D050051:Transient Receptor Potential Channels / Q000037:antagonists & inhibitors*; D014316:Tritium / Q000737:chemistry
chemical_list: C000590221:4-(2'-chloro-6'-hydroxyphenyl)-2-thioxo-3,4-dihydro-1H-indeno(1,2-d)pyrimidin-5(2H)-one; D007192:Indenes; D011743:Pyrimidines; D050051:Transient Receptor Potential Channels; D014316:Tritium
keywords: 3H; NMR; TRPA1; isotopically labeled synthesis