The Hantzsch reaction for nitrogen-13 PET: preparation of [13N]nifedipine and derivatives

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Nitrogen-13 is an attractive but under-used PET radionuclide for labelling molecules of biological and pharmaceutical interest, complementing other PET radionuclides. Its short half-life (t1/2 = 9.97 min) imposes synthetic challenges, but we have expanded the hitherto limited pool of 13N labelling strategies and tracers by adapting the multicomponent Hantzsch condensation reaction to prepare a library of 13N-labelled 1,4-dihydropyridines from [13N]ammonia, including the widely-used drug nifedipine. This represents a key advance in 13N PET radiochemistry, and will serve to underpin the renewed interest in clinical opportunities offered by short-lived PET tracers.
Original languageEnglish
Pages (from-to)4962-4965
Number of pages4
JournalChemical communications (Cambridge, England)
Issue number40
Publication statusPublished - 18 May 2021


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