Synthesis of M4IDP and Optimum Labeling Conditions of 99Tcm-M4IDP
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Abstract
1-Hydroxy-2-(4-methyl-1H-imidazoleyl)-ethylidene-1,1-bisphosphonic(M4IDP)was prepared by three steps of N-alkylation、ester hydrolation and phosphoric acid acylation from the raw material 4-methyl-1H- imidazole. The structures of intermediate and target compounds were identified by Elemental Analysis、IR、MS and 1H NMR. Then M4IDP was directly labeled by Na99TcmO4 to afford 99Tcm-M4IDP. The results showed that the best labeling conditions were 30 minutes reaction time, pH 6,100 μg SnCl2·2H2O, and 5 mg M4IDP. In this condition, the labeling yield was more than 95% and 99Tcm-M4IDP showed good biological stability in vitro.
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