Premium
Radiosynthesis of [ 11 C]nifedipine and [ 11 C]nicardipine
Author(s) -
Wilson Alan A.,
Dannals Robert F.,
Ravert Hayden T.,
Donald Burns H.,
Lever Susan Z.,
Wagner Henry N.
Publication year - 1989
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.2580270513
Subject(s) - nicardipine , chemistry , radiosynthesis , nifedipine , dihydropyridine , alkylation , calcium channel , calcium , organic chemistry , in vivo , catalysis , microbiology and biotechnology , biology
The radiosyntheses of the dihydropyridine (DHP) calcium channel blockers [ 11 C]nifedipine and [ 11 C]nicardipine by alkylation of the appropriate DHP 3‐monocarboxylic acid anion with [ 11 C]iodomethane are described. Isolated radiochemical yields of 30–50% were obtained 25 minutes after the end‐of‐bombardment, with specific activities of 400–1400 mCi/μmol at the end‐of‐synthesis. A variety of positron emitting DHPs with different ester side chains in the 3 and 5 positions on the DHP ring may be prepared by this approach using currently available labelled alkylating agents.