Paper
Synthesis of high specific activity tritium labeled (E)‐6‐(bromomethylene)‐tetrahydro‐3‐(1‐naphthalenyl)‐2H‐pyran‐2‐one as a selective probe for calcium‐independent phospholipase a2
Published Sep 1, 1992 · R. C. Durley, B. Parnas, R. H. Weiss
Journal of Labelled Compounds and Radiopharmaceuticals
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Abstract
The synthesis of (E)-6-(bromomethylene)-tetrahydro-3-([4-3H]-1-naphthalenyl)-2H-pyran-2-one at a specific activity of 24.0 Ci/mmol is described. This probe was synthesized to determine whether (E)-6-(bromomethylene)-tetrahydro-3-(1-naphthalenyl)-2H-pyran-2-one inhibits calcium-independent myocardial phospholipase A2 irreversibly via covalent modification. The material was synthesized in four steps from 1-naphthalene acetic acid via [4-3H]-1-naphthaleneacetic acid. The yield from [4-3H]-1-naphthaleneacetic acid was 29.7%. The radiochemical purity of the HPLC-purified final product was 99.5%.
This study successfully synthesized (E)-6-(bromomethylene)-tetrahydro-3-(1-naphthalenyl)-2H-pyran-2-one, a selective probe for calcium-independent phospholipase A2, with a specific activity of 24.0
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