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Synthesis of carbon-11 labelled calcium channel antagonists

✍ Scribed by M. Holschbach; W. Roden; W. Hamkens

Publisher
John Wiley and Sons
Year
1991
Tongue
French
Weight
392 KB
Volume
29
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

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%).

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