A tin precursor for the synthesis of no-carrier-added [*I]MIBG and [211
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.
Vaidyanathan, G; Affleck, DJ; Alston, KL; Zalutsky, MR
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