A convenient method to produce [(14) C]carbon monoxide and its application to the radiosynthesis of [carboxyl-(14) C]celivarone, [carboxyl-(14) C]SSR149744.

[carboxyl-(14) C]Celivarone was synthesised from barium [(14) C]carbonate with overall radiochemical yields in the range 49-53%. The synthetic route involves [(14) C]carbonylation methodology, which both decreased the number of synthetic steps and increased the yields obtained from previous synthetic routes.

A method for parallel solid-phase synthesis of iodinated analogues of the CB1 receptor inverse agonist rimonabant.

A method for the parallel solid-phase synthesis (SPS) of iodinated analogues of Sanofi-Aventis' type 1 cannabinoid (CB1) receptor inverse agonist rimonabant (acomplia) has been developed. The method allows the synthesis of a range of C3 amide/hydrazide derivatives from a resin-bound C3 ester precursor. The C-Ge linkage to the Hypogel-200 resin is stable to the diversification conditions but allows ipso-iododegermylative cleavage using NaI/NCS even for the products containing the oxidatively labile hydrazide moiety.

A strategy for isotope containment during radiosynthesis--devolatilisation of bromobenzene by fluorous-tagging-Ir-catalysed borylation en route to the 4-phenylpiperidine pharmacophore.

Syntheses of two 4-phenylpiperidines from bromobenzene have been developed involving anchoring to a fluorous-tag, Ir-catalysed borylation, Pd- and Co-catalysed elaboration then traceless cleavage. Although performed using 'cold' (i.e.