Synthesis of carbon‐13 and carbon‐14 labelled triazolo‐1,4‐benzodiazepines
- 1 April 1989
- journal article
- research article
- Published by Wiley in Journal of Labelled Compounds and Radiopharmaceuticals
- Vol. 27 (4) , 407-416
- https://doi.org/10.1002/jlcr.2580270407
Abstract
An efficient two‐step synthesis of 8‐chloro‐1‐methyl‐6‐phenyl‐[3H]‐S‐triazolo‐[4,3‐a][1,4]‐benzodiazepine (alprazolam) and 8‐chloro‐6‐(2‐chlorophenyl)‐1‐methyl‐[3H]‐S‐triazolo‐[4,3‐a][1,4]‐benzodiazepine (triazolam) labelled with carbon‐13 or carbon‐14 from their corresponding hydrazines is reported. The method involves acylation of the appropriate hydrazine using the mixed carbonic anhydride of sodium [13C] or [14C] acetate and isobutylchloroformate under mild conditions. Thermolysis of the resulting acetylhydrazides gave the target carbon‐14 and carbon‐13 labelled compounds in good yields.Keywords
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