| Autor: |
Musachio JL; Division of Nuclear Medicine Sciences, Johns Hopkins Medical Institutions, Baltimore, MD 21205-2179, USA., Keverline KI, Carroll FI, Dannals RF |
| Jazyk: |
angličtina |
| Zdroj: |
Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine [Appl Radiat Isot] 1996 Jan; Vol. 47 (1), pp. 79-81. |
| DOI: |
10.1016/0969-8043(95)00259-6 |
| Abstrakt: |
Here we report the synthesis of 3 beta-(p-trimethylsilylphenyl)tropane-2 beta-carboxylic acid methyl ester, a new, easily prepared precursor for the synthesis of radioiodinated versions of RTI-55. In contrast to the 3 beta-(p-trimethylstannylated) precursor for radioiodination, the aryl silane is prepared directly by the 1,4 addition of p-trimethylsilylphenylmagnesium iodide to anhydroecgonine methyl ester in 49% yield (Scheme 1). Radioiododesilylation proceeded smoothly (approx. 85% radioincorporation after 15 min at room temperature) using 1 microgram of the novel precursor in trifluoroacetic acid and chloramine-T as oxidant. Isolated radiochemical yields for 125I and 123I radiolabelings were 72 and 48%, respectively, with a calculated specific activity for [123I]RTI-55 of > 2000 mCi/mumol. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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