Institution: | a MRC Clinical Sciences Centre, Imperial College School of Medicine, Hammersmith Hospital, Du Cane Road, London W12 0NN, UK b Department of PET and Nuclear Medicine, Royal Prince Alfred Hospital, Missenden Road, Camperdown, NSW 2050 Sydney, Australia c Imaging Research Solutions Ltd, Cyclotron Building, Hammersmith Hospital, Du Cane Road, London W12 0NN, UK |
Abstract: | Two generic radiosynthetic routes for the preparation of 11C-carbonyl]isocyanates have been developed. Reaction of N-organo-sulfinylamines; RNSO, (R = Me, Et, allyl, cyclohexyl and phenyl) with 11C]phosgene gave the corresponding 11C-carbonyl]isocyanates in good radiochemical yield (53–68%) from 11C]phosgene (decay corrected) in ca 16 min from EOB. Alternatively, the reaction of 11C]phosgene with N,N′-organo-ureas; (RNH)2CO, (R = Me, Et, Pr and phenyl) also gave the corresponding 11C-carbonyl]isocyanates in moderate radiochemical yield (9–37%) from 11C]phosgene (decay corrected) in ca 16 min from EOB. For identification, the 11C-carbonyl]organo-isocyanates were derivatized with 1-(2-methoxyphenyl)piperazine in situ to 11C-carbonyl]carboxamides and the position of radiolabelling in the carbonyl group confirmed by 11/13C]co-labeling and subsequent carbon-13 NMR spectroscopy. |