Diethylenetriaminepentaacetic acid (DTPA) and its derivatives have been used in chemistry, biology, medicine and many other fields due to their coordination properties, especially, used as magnetic resonance imaging (MRI) contrast agent. Bifunctional-DTPA ligand can be easily and readily linked to various biomolecules. It is of primary importance for the development high relaxation efficiency and/or targeted MRI contrast agents, but the synthesis of bifunctional-DTPA ligand is rather difficult. In this review, various synthetic methods for synthesizing these compounds are summarized.
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