Tritium labelled 8-chloro-l-[(dimethylamino)methyl]-6-phenyl-4H-striazolo[4,3-a][ 1,4]benzodiazepine was prepared from [3Hlbromomethane and 8chloro-I -[(N-methylamino)methyl]-6-phenyl-4H-s-triazolo[4,3-a][ 1.4lbenzodiazepine. The latter compound was efficiently obtained from 8-chloro-6-phenyl- 4H-s-
The synthesis of betaxolol labelled with tritium at high specific activity
✍ Scribed by John Allen; André Tizot
- Publisher
- John Wiley and Sons
- Year
- 1988
- Tongue
- French
- Weight
- 204 KB
- Volume
- 25
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Department of Chemistry Labelled Compounds and Metabolite Synthesis Group
31, avenue Paul Vaillant-Couturier 92220 BAGNEUX (FRANCE) SmOuRY The synthesis of betaxolol, a new 8-blocking agent. labelled with tritium in high specific activity ('19 Ci/mmol) is described. The tritium was incorporated into the molecule via a catalytic reductive debromination of the 2.6-dibromobetaxolol precursor in the presence of tritium gas. This labelled compound has been used in receptor binding studies and also in studying the release of betaxolol from rat atrial slices on electrical stimulation.
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