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A tin precursor for the synthesis of no-carrier-added [*I]MIBG and [211At]MABG

Publication ,  Journal Article
Vaidyanathan, G; Affleck, DJ; Alston, KL; Zalutsky, MR
Published in: Journal of Labelled Compounds and Radiopharmaceuticals
January 1, 2007

Radioiodinated MIBG has shown considerable promise as an imaging agent for cardiac and oncologic applications, and also as a targeted radio therapeutic for treating patients with neuroendocrine tumors. This radiolabeled agent, synthesized at a no-carrier-added level, has demonstrated advantages over the carrier-added preparation in preliminary clinical studies. Earlier we developed a silicon precursor from which both radioiodinated MIBG and the α-particle-emitting 211At analog [211At]MABG could be synthesized at a no-carrier-added level. In order to increase the practicality of this approach, we have developed a synthesis of a tin precursor in two steps from a readily available starting material. This tin precursor, N, N′-bis(tert-butyloxycarbonyl)-3-(trimethylstannyl)benzylguanidine (Bis-Boc MTMSBG) was evaluated for the synthesis of n.c.a. [*I]MIBG and [ 211At]MABG via halodestannylation. The radiochemical yields were 83 ± 9% (n = 7), 30 ± 21% (n = 2), 77 ± 2% (n = 2), and 66 ± 7% (n = 4) for labeling with 131I, 124I, 125I, and 211At, respectively. Copyright © 2007 John Wiley & Sons, Ltd.

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Published In

Journal of Labelled Compounds and Radiopharmaceuticals

DOI

EISSN

1099-1344

ISSN

0362-4803

Publication Date

January 1, 2007

Volume

50

Issue

3

Start / End Page

177 / 182

Related Subject Headings

  • Medicinal & Biomolecular Chemistry
  • 3405 Organic chemistry
  • 1115 Pharmacology and Pharmaceutical Sciences
  • 0305 Organic Chemistry
 

Citation

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Vaidyanathan, G., Affleck, D. J., Alston, K. L., & Zalutsky, M. R. (2007). A tin precursor for the synthesis of no-carrier-added [*I]MIBG and [211At]MABG. Journal of Labelled Compounds and Radiopharmaceuticals, 50(3), 177–182. https://doi.org/10.1002/jlcr.1243
Vaidyanathan, G., D. J. Affleck, K. L. Alston, and M. R. Zalutsky. “A tin precursor for the synthesis of no-carrier-added [*I]MIBG and [211At]MABG.” Journal of Labelled Compounds and Radiopharmaceuticals 50, no. 3 (January 1, 2007): 177–82. https://doi.org/10.1002/jlcr.1243.
Vaidyanathan G, Affleck DJ, Alston KL, Zalutsky MR. A tin precursor for the synthesis of no-carrier-added [*I]MIBG and [211At]MABG. Journal of Labelled Compounds and Radiopharmaceuticals. 2007 Jan 1;50(3):177–82.
Vaidyanathan, G., et al. “A tin precursor for the synthesis of no-carrier-added [*I]MIBG and [211At]MABG.” Journal of Labelled Compounds and Radiopharmaceuticals, vol. 50, no. 3, Jan. 2007, pp. 177–82. Scopus, doi:10.1002/jlcr.1243.
Vaidyanathan G, Affleck DJ, Alston KL, Zalutsky MR. A tin precursor for the synthesis of no-carrier-added [*I]MIBG and [211At]MABG. Journal of Labelled Compounds and Radiopharmaceuticals. 2007 Jan 1;50(3):177–182.
Journal cover image

Published In

Journal of Labelled Compounds and Radiopharmaceuticals

DOI

EISSN

1099-1344

ISSN

0362-4803

Publication Date

January 1, 2007

Volume

50

Issue

3

Start / End Page

177 / 182

Related Subject Headings

  • Medicinal & Biomolecular Chemistry
  • 3405 Organic chemistry
  • 1115 Pharmacology and Pharmaceutical Sciences
  • 0305 Organic Chemistry