Method for preparing precursor of radioactive...

Organic compounds -- part of the class 532-570 series – Organic compounds – Heavy metal containing

Reexamination Certificate

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C556S107000

Reexamination Certificate

active

08076499

ABSTRACT:
A method for preparing a precursor of radioactive 3-iodobenzylguanidine- N,N′-bis(tert-butyloxycarbonyl)-3-(tri-n-butyltin)benzylguanidine) (MSnBG) is revealed. The method includes following steps. Firstly, obtain 3-iodobenzylguanidine bicarbonate by an addition reaction between 3-iodobenzylamine hydrochloride and cyanamide. Use di-tert-butyl dicarbonate as a protecting agent for NH group and convert 3-iodobenzylguanidine bicarbonate into N,N′-bis(tert-butyloxycarbonyl)-N-(3-iodobenzyl) guanidine. At last, under catalysis of bis(triphenylphosphine) palladium dichloride, obtain a final product MSnBG by a substitution reaction between N,N′-bis(tert-butyloxycarbonyl)-N-(3-iodobenzyl) guanidine and bis(tri-n-butyltin). MSnBG is used in no-carrier-added synthesis of [*l]MIBG.

REFERENCES:
Vaidynathan et al, Journal of Labeled compounds and Radiopharmaceuticals, A Tin Precursor for the Synthesis of No-carrier-added [*I]MIBG and [211At]MABG, 2007, 50, pp. 177-182.

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