Novel and facile methods for the synthesis of DTPA-mono-amide: a new completely revised strategy in radiopharmaceutical chemistry |
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Authors: | Mehdi Shafiee Ardestani Ali Jabbari Arabzadeh Zahra Heidari Amirreza Hosseinzadeh Hamidreza Ebrahimi Elham Hashemi Mona Mosayebnia Mohammad Shafiee-Alavidjeh Abbas Alavi Mohammad Hossein Babaei Arman Rahmim Seyed Esmaeil Sadat Ebrahimi Massoud Amanlou |
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Affiliation: | 1. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran 2. Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran 3. Division of Nuclear Medicine, Department of Radiology, School of Medicine, Pennsylvania University of Medical Sciences, Philadelphia, PA, USA 4. Radioisotope Research Center, Atomic Energy Organization of Iran, Tehran, Iran 5. Department of Radiology, School of Medicine, Johns Hopkins University, Baltimore, MD, USA
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Abstract: | DTPA is a very strong metal chelator widely utilized in radiopharmaceutical chemistry for conjugation of chemicals which do not have enough potency for direct metalo-labeling and also to manage toxic radioactive materials such as plutonium, americium, and curium. It is difficult to conjugate DTPA to an amine group in a singular direction and such reactions usually also coincidently produce a mixture of DTPA-bis-amides and DTPA-mono-amide resulting in considerable insufficiencies/difficulties in synthesis and especially yield/separation procedures. In this paper, novel methods for the exclusive synthesis of DTPA-mono-amide have been established which extensively reduce the difficulties otherwise encountered and increase the reaction’s yield considering the green chemistry approaches. This is expected to be of interest to radiopharmaceutical researchers interested in the DTPA (Radio)-metallic-conjugate. Overall, this paper provides a framework to achieve a higher degree of propriety from DTPA as a chelator to conjugate to the chemical compounds. |
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