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
Autor: | Barry L. Parnas, Randy H. Weiss, Richard C. Durley |
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Rok vydání: | 1992 |
Předmět: |
chemistry.chemical_classification
biology Bicyclic molecule Chemistry Stereochemistry Organic Chemistry Biochemistry Analytical Chemistry chemistry.chemical_compound Acetic acid Phospholipase A2 Pyran Yield (chemistry) Drug Discovery biology.protein Radiology Nuclear Medicine and imaging Tritium Specific activity Spectroscopy Lactone |
Zdroj: | Journal of Labelled Compounds and Radiopharmaceuticals. 31:685-691 |
ISSN: | 0362-4803 |
Popis: | 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%. |
Databáze: | OpenAIRE |
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