The synthesis of 14С-etoxozepam ad determination of it`s main physico-chemical and radiochemical properties

  • V.I. Pavlovsky -
  • E.A. Semenishina -
  • V.B. Larionov -
  • N.A. Zhukova -
Keywords: radioactive labeled compounds, 1,4-benzodiazepine derivatives, 14C-etoxozepam

Abstract

The aim of this work was synthesis, identification and radiochemical characterization of 3-ethoxy-7-bromo-5phenyl-1,2-dihydro-3Н-1,4-benzodiazepine-2-one.

The 14C-labeled compound (14С-etoxozepam) was synthesized from 7-bromo-5-phenyl-3-chloro-1,2-dihydro-3Н-1,4-benzodiazepine-2-one with 2[14С] – ethyl alcohol. The physics chemical constants (Тmelt., IR-, 1Н-NMR- and mass-spectra) are identical to the standard sample.

The specific activity of the sample is 0,199 ± 0,001 Cu/mol (0,7 MBk/mol), and radiochromatographic purity – 96,2 %.

References

1. Golovenko N.Ya., Zhuk OV, Zinkovsky V.G. et al. Calculations of pharmacokinetic parameters of drugs (linear partial models). Guidelines. - Kiev. - Avicena, 2003. - 20 p.
2. Golovenko N.Ya., Zinkovsky V.G., Yakubovskaya L.N. Synthesis of radiolabelled derivatives of 1,4-benzodiazepine and determination of the structure of their metabolites // Ukr. chemical journals - 1999. - Vol. 65, No. 9. - p. 34-44.
3. Chadr G. Radioimmunological methods. M .: Mir, 1981. - 246 p.
4. Sozinov V.A., Rudenko OP, Golovenko N.Ya. et al. Synthesis and correlation between the structure and pharmacological activity of 1,3-dihydro-2H-1,4-benzodiazepin-2-one derivatives. // Chem.-farm. journals - 1984. - №10. - p. 67 - 71.
5. Veshurova ON, Kolinovskaya G.Ya., Takhanaev A.A. et al. Introduction of the tritium label into alkaloids by the method of heterogeneous catalytic exchange. In the book. Biologically active compounds labeled with radioactive isotopes. M .: Medicine, 1985. - p. 14 - 15.
6. Golovenko N.Ya, Rev. E.V. Pharmaco-toxicological characteristics of gidazepam and its metabolites. // Modern problems of pharmacology and toxicology. - 2007. - № 4. - p. 41 - 44.
7. Synthesis of 14C-gidazepamu yogo potentsiyynyh metabolite. / M.Ya.Golovenko, V.I.Pavlovsky, K.V.Prepodobna, V.B.Larionov, K.O.Semenіshina // Ukrainica Bioorganica ACTA. - 2007. - pp. 20 - 23.
Published
2019-03-18
How to Cite
Pavlovsky, V., Semenishina, E., Larionov, V., & Zhukova, N. (2019). The synthesis of 14С-etoxozepam ad determination of it`s main physico-chemical and radiochemical properties. Farmatsevtychnyi Zhurnal, (2), 43-49. Retrieved from https://pharmj.org.ua/index.php/journal/article/view/529
Section
Original Articles