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- Title
Synthesis of 2[<sup>14</sup>C]-3-propoxy-1.4-benzdiazepine-2-one for pharmacokinetic research.
- Authors
Pavlovsky, V. I.; Larionov, V. B.; Valivodz, I. P.
- Abstract
The aim of the work was synthesis of 214C-7-bromo-5-(o-chlorophenyl)-3-propoxy-1.2-dihydro-3H-1.4-benzdiazepine-2-one (BD-007), determination of its radiological properties as well as the possibility of use in pharmacological studies (isolation and determination in biological samples). BD-007 isotope 14C labeling was made at «2» position of heteroring, which remains in molecule after most of metabolic transformations, using 114C-glycine (via condensation of corresponding benzophenone with glycine chloroanhydride hydrochloride and further reaction of halogen derivative of 1.4-benzdiazepine with n-propyl alcohol). Radiochromatographic purity of obtained 2[14C]-7-bromo-3-propoxy-5-(2-chlorophenyl)-1,3-dihydro[е][1,4]diazepine-2-one substance was 66 % and specific activity 2,68 µCu/mol (0,16 kBk/mol), that is sufficient for primary studies in pharmacokinetics and metabolism. In model experiments the quantity of subsequent extractions and extragent/sample volumes ratio for isolation of radioactivity with required accuracy level (90, 95 or 99 %) were calculated. The determined analytical properties (variation coefficient ωs, 3,33 %, relative error, ε, 9,53 %) allow using of this method in pharmacokinetic studies.
- Publication
Ukrainica Bioorganica Acta, 2015, Vol 13, Issue 2, p26
- ISSN
1814-9758
- Publication type
Article