METHOD FOR PREPARING PRECURSOR OF RADIOACTIVE 3-IODOBENZYLGUANIDINE

A method for preparing a precursor of radioactive 3-iodobenzylguanidine-N,N′-bis(tert-butyloxycarbonyl)-3-(tri-n-butyltin)benzylguanidine) (MSnBG) is revealed. The MSnBG is a precursor of [*I]MIBG that is used as radioactive imaging agents and antineoplastic drugs. The method includes following step...

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Bibliographic Details
Main Authors HSU CHENG-FANG, LIN CHENG-HSIEN, LIN TSYH-LANG, LIU SHOW-WEN
Format Patent
LanguageEnglish
Published 17.02.2011
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
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Summary:A method for preparing a precursor of radioactive 3-iodobenzylguanidine-N,N′-bis(tert-butyloxycarbonyl)-3-(tri-n-butyltin)benzylguanidine) (MSnBG) is revealed. The MSnBG is a precursor of [*I]MIBG that is used as radioactive imaging agents and antineoplastic drugs. 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 [*I]MIBG. The [*I]MIBG obtained by this method has better effect on neuroblastoma treatment than that obtained by conventional, carrier-added method.
Bibliography:Application Number: US20090540448