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Preparation of carbon‐11 labelled prazosin, a potent and selective α 1 ‐adrenoreceptor antagonist
Author(s) -
Ehrin Erling,
Luthra Sajinder K.,
Crouzel Christian,
Pike Victor W.
Publication year - 1988
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580250209
Subject(s) - prazosin , chemistry , antagonist , amine gas treating , yield (engineering) , azetidine , in vivo , radiochemistry , nuclear chemistry , medicinal chemistry , stereochemistry , organic chemistry , receptor , biochemistry , materials science , microbiology and biotechnology , metallurgy , biology
The α 1 ‐adrenoreceptor antagonist, Prazosin : 2‐[4‐(2‐furoyl) piperazin‐1‐yl]‐4‐amino‐6,7‐dimethoxyquinazoline, has been labelled with carbon‐11 for in vivo studies of α 1 ‐adrenoreceptors using positron emission tomography. The preparation of [2‐ 11 C] furoyl chloride, from cyclotron‐produced [ 11 C] carbon dioxide, and its reaction with the secondary amine, 2‐(piperazin‐1‐yl)‐4‐amino‐6,7‐dimethoxyquinazoline, provides a fast (35 min) route to carbon‐11 labelled prazosin in high radiochemical yield (30‐40 %, decay‐corrected) with high specific activity (26‐37 GBq/μmol, 0.7‐1.0 Ci/μmol).