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Synthesis of 14 C‐labelled 10‐[3‐(dimethylamino)‐propyl]‐2‐nitrodibenz [b,f] [1,4] oxazepin‐11‐(10 H)‐one (nitroxazepine)hydrochloride
Author(s) -
Maller R. K.,
Nagarajan K.
Publication year - 1983
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.2580201205
Subject(s) - chemistry , paraformaldehyde , yield (engineering) , hydrochloride , derivative (finance) , nitrogen atom , potassium cyanide , carbon atom , ring (chemistry) , stereochemistry , cyanide , medicinal chemistry , potassium , organic chemistry , materials science , economics , financial economics , metallurgy
For pharmacokinetic and metabolism studies in animals and humans, nitroxazepine, an antidepressant, was labelled with carbon‐14 at the 11‐position of the dibenzoxazepine ring system in an overall yield of 12% starting with potassium [ 14 C] cyanide. The labelled preparation had a specific activity of 0.95 μCi/mg. 14 C Label was also introduced in the methyl group of the terminal nitrogen atom in the side chain of nitroxazepine, starting from its des‐methyl derivative and using [ 14 C] paraformaldehyde. In this case the overall yield of the final compound was 20%, and its specific activity 1.84 μCi/mg.