Rapid one-pot radiosynthesis of [carbonyl-¹¹C]formamides from primary amines and [¹¹C]CO₂.

ABSTRACT:

Background

Formamides are common motifs of biologically-active compounds (e.g. formylated peptides) and are frequently employed as intermediates to yield a number of other functional groups. A rapid, simple and reliable route to [carbonyl-¹¹C]formamides would enable access to this important class of compounds as in vivo PET imaging agents.

Results

A novel radiolabelling strategy for the synthesis of carbon-11 radiolabelled formamides ([¹¹C]formamides) is presented. The reaction proceeded with the conversion of a primary amine to the corresponding [¹¹C]isocyanate using cyclotron-produced [¹¹C]CO₂, a phosphazene base (2-tert-butylimino-2-diethylamino-1,3-dimethylperhydro-1,3,2-diazaphosphorine, BEMP) and phosphoryl chlorid

SUBMITTER: Luzi F 

PROVIDER: S-EPMC7462944 | biostudies-literature | 2020 Sep

REPOSITORIES: biostudies-literature