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Synthesis of carbon‐11 labelled calcium channel antagonists
Author(s) -
Holschbach M.,
Roden W.,
Hamkens W.
Publication year - 1991
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.2580290408
Subject(s) - chemistry , nisoldipine , nitrendipine , nifedipine , chemical synthesis , calcium , hydrolysis , calcium channel , carbon 14 , potassium , organic chemistry , biochemistry , physics , quantum mechanics , in vitro
A useful synthetic approach to carbon‐11 labelled 1,4‐dihydropyridines is described. Carbon‐11 labelled calcium channel antagonists 11 C‐Nifedipine, 11 C‐Nisoldipine, 11 C‐Nitrendipine and 11 C‐CF 3 ‐Nifedipine were synthesized by a modified Hantzsch method using protected carboxy functions. Deprotection of the carboxylic acids by alkaline hydrolysis followed by conversion into the corresponding potassium salts and subsequent methylation with 11 CH 3 I produced the labelled compounds in very good chemical and radiochemical yields (94%).