A direct synthesis of a bifunctional chelating agent for radiolabeling proteins

Article abstract of DOI:10.1016/S0040-4039(00)79202-1

A convenient synthesis of a bifunctional derivative of the ligand NOTA is described. The synthesis offers advantages over current literature methods for making similar molecules by starting with the easily prepared ortho-amide of 1,4,7-triazacyclanonane which can be sequentially alkylated to provide a bifunctional NOTA derivative in 9% yield overall. The replacement of preparative HPLC with simple ion-exchange chromatography provides analytically pure ligand suitable for clinical applications.