Radiohalogenation of terguride via organotin intermediate

New (radio)halogen derivatives of 1-allylterguride have been prepared by method of destannylation-halogenation. 1-Alylterguride shows relatively high binding affinity, which can be used in the case of its radiolabeled derivatives with imaging methods like PET or SPET in studies of properties of receptor's binding places and ligand affinity. The (radio)halogenation was performed via organotin precursors: 1-tributylstannyl-3-chlorprop-1-ene and 2-tributylstannyl-3-chloroprop-1-ene, which were prepared from appropriate alcohols. Linkers of the tin group were used for alkylation of N1 of terguride both under microwave irradiation and under conventional heating. In the last step (destannylation-halogenation), fluoro-, bromo- and iododerivatives as well as 125 I iodo- and 82 Br bromoderivatives of 1-allylterguride were obtained.