TY - JOUR
T1 - Novel and facile methods for the synthesis of DTPA-mono-amide
T2 - A new completely revised strategy in radiopharmaceutical chemistry
AU - Ardestani, Mehdi Shafiee
AU - Arabzadeh, Ali Jabbari
AU - Heidari, Zahra
AU - Hosseinzadeh, Amirreza
AU - Ebrahimi, Hamidreza
AU - Hashemi, Elham
AU - Mosayebnia, Mona
AU - Shafiee-Alavidjeh, Mohammad
AU - Alavi, Abbas
AU - Babaei, Mohammad Hossein
AU - Rahmim, Arman
AU - Ebrahimi, Seyed Esmaeil Sadat
AU - Amanlou, Massoud
N1 - Funding Information:
Acknowledgments This study was supported by Research Council of the Tehran University of Medical Sciences. We wish to gratefully acknowledge the efforts of Dr. F. Nabati, Prof. M. Izaddoost and all technicians who provided support in the course of this study.
PY - 2010/2
Y1 - 2010/2
N2 - 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.
AB - 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.
KW - DTPA
KW - DTPA-conjugate
KW - Green chemistry
KW - Radiopharmaceutical chemistry
KW - Sonication
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U2 - 10.1007/s10967-009-0414-y
DO - 10.1007/s10967-009-0414-y
M3 - Article
AN - SCOPUS:77949265481
SN - 0236-5731
VL - 283
SP - 447
EP - 455
JO - Journal of Radioanalytical and Nuclear Chemistry
JF - Journal of Radioanalytical and Nuclear Chemistry
IS - 2
ER -