[en] 64Cu (t1/2 = 12.7 h; β+ 0.653 MeV, 17.4%; β-: 0.578 MeV, 39%) is a radionuclide of high interest for nuclear medicine. 64Cu has already been utilized for research purposes due to its favorable decay characteristics and its ability to be produced at high specific activity. Bispidines and azamacrocycles containing pyridine pendant arms form thermodynamically stable complexes with copper (II). These chelating agents possessing an additional linker group provide an attractive lead for labeling biomolecules with copper radionuclides. Experimental: First experiments to adapt the described 64Cu-production process at a PET cyclotron CYCLONE 18/9 were performed. 10 MeV protons and a proton beam current of 10 μA for 15 to 60 min were used. The yields of the 64Ni(p, n) 64Cu nuclear reaction were comparable to reference values [179-331 MBq/μA/h versus 185-248 MBq/μA/h]. Two novel ligands with carboxylic groups a hexadentate bispidine 1 and a derivative of 1,4,7-triazacyclononane (TACN) 2 were prepared. Labeling experiments of these ligands with 64Cu2+ indicated the rapid formation of stable 64Cu-complexes under mild conditions. The bioconjugates 3 and 4 were obtained by coupling the bombesin (BN) derivate βAla-βAla- [Cha13, Nle14] BN (7-14) to the ligands 1 and 2 (HBTU, DIPEA, DMF, r.t.). Results and Discussion: The bioconjugation of 1 and 2 to a bombesin derivative was successfully achieved via amide formation to give 3 and 4. The free ligands and the bioconjugates were labeled with 64Cu2+ and the resulting complexes were found to be stable in the presence of a large excess of competing ligands such as cyclam and even in rat plasma. Conclusion: The bispidine ligand 1, the TACN derivative 2 and their bombes in bioconjugates 3 and 4 are able to form complexes with high stability. These bifunctional chelating agents may be attractive candidates for the development of new copper radiopharmaceuticals for diagnosis (64Cu) and therapy (67Cu). Preliminary studies on the bio-distribution of 64Cu-complexes of 3 and 4 are currently underway