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Hammerschmidt, F; Kvaternik, H; Schweifer, A; Mereiter, K; Aigner, RM; .
Improved Synthesis of No-Carrier-Added [I-star]MIBG and Its Precursor.
SYNTHESIS-STUTTGART. 2012; 44(21): 3387-3391.
Doi: 10.1055/s-0032-1316789
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- Co-authors Med Uni Graz
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Aigner Reingard
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Kvaternik Herbert
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- Abstract:
- 3-(Trimethylstannyl)benzyl alcohol was coupled in a Mitsunobu reaction with bis(Boc)-guanidine to give bis(Boc)-protected 3-(trimethylstannyl) benzylguanidine used as precursor for [*I]MIBG. Radioiodination with [I-131]iodine generated from [I-131]NaI and chloramine-T, removal of Boc groups, and purification by HPLC gave no-carrier-added tracer [*I]MIBG (81% radiochemical yield, 99% chemical purity) used for imaging tumors of neuroendocrine origin. The structures of bis(Boc)-guanidine and bis(Boc)-protected 3-(trimethylstannyl) benzylguanidine were secured by single crystal X-ray structure analyses.
- Find related publications in this database (Keywords)
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Mitsunobu reaction
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electrophilic aromatic substitution
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medicinal chemistry
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[I-131]iodine
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halogenation