Citation

Durley RC, Parnas BL, Weiss RH. Journal of Labelled Compounds and Radiopharmaceuticals 1992; 31(9): 685-691.

Copyright

(Copyright © 1992)

DOI

10.1002/jlcr.2580310907

PMID

unavailable

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%. Copyright © 1992 John Wiley & Sons, Ltd.

Language: en

Keywords

article; controlled study; unclassified drug; enzyme inhibition; drug synthesis; suicide substrate; heart muscle; isotope labeling; inhibition; (E)‐6‐(bromomethylene)‐tetrahydro‐3‐([4‐3H]‐1‐naphthalenyl)‐2H‐pyran‐2‐one; delta bromomethylene alpha (1 naphthyl) delta valerolactone; haloenol lactones; myocardial phospholipase A2; phospholipase a2; pyran derivative; tritium