CATALYTIC SYNTHESIS OF AMINO COMPOUNDS, INTERMEDIATES FOR THE SYNTHESIS OF PHARMACEUTICAL SUBSTANCES

DOI: https://doi.org/10.29296/25419218-2018-02-03
Issue: 
2
Year: 
2018

E.L. Kuzmicheva, PhD; Professor N.V. Pyatigorskaya, PhD; Professor E.A. Sapozhnikova, PhD I.M. Sechenov First Moscow State Medical University (Sechenov University); 2-4, Bolshaya Pirogovskaya St., Moscow 119991, Russian Federation

One of the expected outcomes of the Pharma-2020 strategy is to organize the production of substances on the territory of the Russian Federation. The paper gives information on the design and use of catalysts for the synthesis of amino compounds and the results of investigations of the activity of various catalysts, mostly oxide and metal ones, on hydrogenation of aliphatic nitro compounds. It shows the advantage of palladium-based catalysts over nickel skeleton catalysts. The development of their production technology allows one to create an environmentally pure technology, to improve the quality of the prepared product, and to standardize the catalyst. Palladium catalysts can be used repeatedly (over 50 times), which will be able to create a continuous hydrogenation process on granulated catalysts at a later date. The designed palladium catalysts are used in the production of folic acid (hydrogenation of p-nitrobenzoyl-L-glutamic acid and 2,4-diamino-5-isonitroso-6-oxopyrimidine), theophylline (1,3-dimethyl-4,5-aminouracil), theobromine (3-methyl-4,5-aminouracil), anesthesin, droperidol, etc.

Keywords: 
pharmaceutical substances
hydrogenation
nitro compounds
amino compounds
palladium and nickel catalysts
activity of catalysts

References: 
  1. Hoseva E.N Sostoyanie farmacevticheskoy otrasli na sovremennom e`tape. Kachestvennaya klinicheskaya praktika, 2014; 3: 117–45.
  2. Kovaleva E.L. Sovershenstvovanie metodologicheskih podhodov k obespecheniyu kachestva i standartizacii substanciy i preparatov v lekarstvennoy forme «tabletki». Avtoref. … dokt. farm. nauk. M., 2010; 48.
  3. Prikaz Minpromtorga RF № 916 ot 14.06.2013 s izmeneniyami ot 18.12.2015 g. «Ob utverzhdenii Pravil nadlezhashhey proizvodstvennoy praktiki».
  4. Ob utverzhdenii Koncepcii Federal`noy celevoy programmy «Razvitie farmacevticheskoy i medicinskoy promyshlennosti Rossiyskoy Federacii na period do 2020 goda i na dal`neyshuyu perspektivu» Rasporyazhenie Pravitel`stva RF № 41 ot 11.10.2010g.
  5. O Federal`noy celevoy programme «Razvitie farmacevticheskoy i medicinskoy promyshlennosti Rossiyskoy Federacii na period do 2020 goda i na dal`neyshuyu perspektivu». Postanovlenie Pravitel`stva RF № 91 ot 17.02.2011 g. Rossiyskaya gazeta № 57 ot 18.03.2011 g.
  6. Farmacevticheskaya razrabotka. Koncepciya i prakticheskie rekomendacii. Pod red. S.N. Bykovskogo. M.: Pero, 2015.
  7. Obzor rynka promyshlennosti katalizatorov v Rossii. InfoMayn issledovatel`skaya gruppa. Ob``edinenie nezavisimyh e`kspertov v oblasti mineral`nyh resursov, metallurgii i himicheskoy promyshlennosti. M., 2010.
  8. Jap. Sposob uluchsheniya harakteristiki katalizatora. Energy and Technol. Intell., 1991; 9: 36. RZh «Himiya», 1993; 8: 8L109.
  9. Bal`zhinimaev B.S., Simonova L.G. Katalizatory na osnove steklovoloknistyh nositeley. Adsorbcionnye i kataliticheskie svoystva Pt i Pd nanesennyh na steklovidnye nositeli v reakciyah selektivnogo gidrirovaniya acetilenov. Kinetika i kataliz, 2002, 43/4: 584–6.
  10. Titova Yu.Yu. Rol` alyuminiy- i borsoderzhashhih soedineniy v formirovanii nanorazmernyh katalizatorov gidrirovaniya na osnove kompleksov palladiya. Avtoref. … dokt. him. nauk. 2013; 48.
  11. Tolstikov G.A., Popova I.L., Borisova E.Ya., Komarov V.M., Cherkashin M.I. Kataliticheskie prevrashheniya ciklogeksadienov v prisutstvii rodievogo katalizatora Rh/S. Doklady RAN, 1993, 331/1, 58–61.
  12. Maylyubaev B.T., Ualizhanova A. Vliyanie rastvoriteley na prevrashhenie anilina v atmosfere vodoroda v prisutstvii katalizatorov. ZhPH, 1993, 66 (10); 2282.
  13. Sass A.S., Antonova N.A., Popova N.M. Vosstanovlenie vodorodom Pt-Re-Ce-katalizatorov na okside alyuminiya. Kinetika i kataliz,1996; 36 (1): 112–5.
  14. Kuz`micheva E.L. Fiziko-himicheskie osnovy sinteza palladievogo katalizatora dlya polucheniya termolabil`nyh soedineniy slozhnoy struktury. Avtoref. … dokt. tehn. nauk, M., 2005; 48.