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Article
Modernization of the Synthesis and Anti-Inflammatory Activity of 4,10-di(2-Ethoxyacetyl)-2,6,8,12-Tetraacetyl-2,4,6,8,10,12-Hexaazaisowurtzitane – An Innovative Non-Narcotic Analgesic
A modified method for the synthesis of a promising non-narcotic analgesic agent of the hexaazaisowurtzitane class with pronounced anti-inflammatory activity is described. Methods for reducing the cost of the t...
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Article
Hydrogenation of Dinitrobenzenes to Corresponding Diamines Over Cu–Al Oxide Catalyst in a Flow Reactor
The catalytic hydrogenation of dinitroaromatic compounds is an important reaction for the production of phenylenediamine derivatives, which are widely used in industry. In this work, the catalytic properties o...
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Article
Selective Catalytic Hydrodebromination of 2,3,4,5-Tetrabromothiophene with Hydrogen on a Palladium Catalyst
A way of hydrodebrominating 2,3,4,5-tetrabromothiophene (1) to 3,4-dibromothiophene (2) on a 5% Pd/Sibunit catalyst is proposed. The effect of solvent, alkaline agent, temperature, and concentration of 1 on the y...
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Article
Synthesis and Biological Activity of 4-(3,4-Dibromothiophenecarbonyl)-2,6,8,10,12-Pentaacetyl-2,4,6,8,10,12-Hexaazaisowurtzitane: A New Non-Narcotic Analgesic of the Hexaazaisowurtzitane Class
A method for production of a promising non-narcotic analgesic of the hexaazaisowurtzitane class is developed. Data on the physicochemical characteristics and conditions for obtaining the target substance are p...
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Article
A Comparative Study of the Hydrogenation of 1,3,5-Trinitrobenzene and 2,4,6-Trinitrotoluene over a Copper–Alumina Catalyst in a Flow Reactor
The catalytic properties of a copper–alumina catalyst prepared from double layered hydroxide have been studied in the hydrogenation of 1,3,5-trinitrobenzene (TNB) and 2,4,6-trinitrotoluene (TNT) in a flow reac...
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Article
Antinociceptive Effect of Ethowurtzine, a New Compound from the Class of Hexaazaizowurzitane
Analysis of specific pharmacological activity evaluated high antinociceptive efficacy of the first synthesized compound 10-di(ethoxyacetyl)-2,6,8,12-tetraacetyl-2,4,6,8,10,12-hexaazatetracyclo[5,5,0,03,11,05,9]do...
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Article
Promising New Salt of Oseltamivir
A synthetic method for the promising new drug oseltamivir ethoxysuccinate is described in detail. Various conditions for obtaining the target substance are considered. Its complete physicochemical characterist...
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Article
Some Aspects of Investigation of the Central Mechanism of Antinociceptive Effect of a New Analgetic from the Hexaazaisowurtzitane Group
Possible involvement of μ1- and κ-opioid receptors and cannabinoid type 1 receptors (CB1) into the mechanism of analgesic activity of the experimental drug product “Thiowurtzine, (capsule 120 mg)” synthesized on ...
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Article
Synthesis and Analgesic Activity of 4,10-Bis((±)-5-Benzoyl-2,3-Dihydro-1hpyrrolo[1,2-a]Pyrrole-1-Carbonyl)-2,6,8,12-Tetraacetyl-2,4,6,8,10,12-Hexaazatetracyclo[5,5,03,11,05,9]Dodecane
A method of preparing the potential analgesic substance 4,10-bis((±)-5-benzoyl-2,3-dihydro-1H-pyrrolo-[1,2-a]pyrrole-1-carbonyl)-2,6,8,12-tetraacetyl-2,4,6,8,10,12-hexaazatetracyclo[5,5,03,11,05,9]dodecane is des...
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Article
Pharmacokinetics of a New Analgesic on the Basis of Hexaazaisowurtzitane Derivative
We studied pharmacokinetics of a new analgesic based on a hexaazaisowurtzitane derivative (thiowurtzine, TWZ). A method for measuring TWZ in organs and tissues by HPLC/MS/MS was developed and validated. The se...
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Article
Development of Technology and Equipment for Enisamium Iodide Drying
A methodological approach to selecting the optimal drying method for enisamium iodide, an antiviral agent with a broad spectrum of pharmacological activities, is considered. A vacuum drying method in an appara...
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Article
Analgesic Activity of Hexaazaisowurtzitane Derivatives
Pronounced analgesic activity of the innovative compound 4-(3,4-dibromthiophencarbonyl)-2,6,8,12-tetraacethyl-2,4,6,8,10,12hexaazatetracyclo[5,5,0,03, 11,05, 9] dodecane (thiowurtzine) was observed in the thermal...
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Article
Anti-Ischemic Activity of n-Tyrozol under Conditions of Repeated Transient Myocardial Ischemia in Rats
We studied anti-ischemic activity of n-tyrozol under conditions of repeated transient myocardial ischemia in rats caused by repeated (5×3 min) occlusion of the left coronary artery. n-Tyrozol administered intrape...
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Article
Synthesis of new N-polysubstituted oxaazaisowurtzitanes by acid-catalyzed condensation of sulfonamides with glyoxal
By application of acid-catalyzed condensation of propane-2-, benzene- and methanesulfonamides with glyoxal a series of new derivatives of oxaazaisowurtzitanes were obtained, in particular, new heterocyclic sys...
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Article
Nitrolysis of 2,6,8,12-tetraacetyl-4,10-dibenzyl-2,4,6,8,10,12-hexaazatetracyclo[5.5.0.03,11.05,9]dodecane
Nitrolysis of 2,6,8,12-tetraacetyl-4,10-dibenzyl-2,4,6,8,10,12-hexaazatetracyclo-[5.5.0.03,11.05,9]dodecane results in the substitution of benzyl groups by the nitro groups with the formation of 2,4,6,8,10,12-hex...
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Article
An unusual reduction route of 2,4,6-trinitrobenzoic acid under conditions of aqueous-phase hydrogenation over Pd/Sibunit catalyst
For the first time it was established that the catalytic hydrogenation of 2,4,6-trinitrobenzoic acid to 1,3,5-triaminobenzene can proceed via the formation of aromatic hydroxyamines and cyclohexane-1,3,5-trione t...
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Article
p-Tyrosol: a new synthetic method and new types of pharmacological activity
A new method for the synthesis of p-tyrosol, i.e., 2-(4-hydroxyphenyl)ethanol, has been developed, which considerably simplified the process of preparation of this pharmaceutical substance. The method includes ni...
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Article
A search for raw materials for the isolation of shikimic acid
The content of shikimic acid in the vegetative parts of a number of plants growing in the Altai Territory has been studied. The greatest content of shikimic acid (about 1.5%) was found in the coniferous needle...
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Article
New syntheses of [1,2,5]oxadiazolo[3,4-e][1,2,3,4]tetrazine 4,6-dioxide
New methods were developed for the synthesis of [1,2,5]oxadiazolo[3,4-e][1,2,3,4]tetrazine 4,6-dioxide from 4-(tert-butyl-NNO-azoxy)-N-nitro-1,2,5-oxadiazol-3-amine or its alkali metal salts and acid anhydrides (...
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Article
Facile method for the synthesis of oseltamivir phosphate
A ten-step scheme for the preparation of an antiviral agent, ethyl (3R,4R,5S)-4-acetylamino-5-amino-3-(pent-3-yloxy)cyclohex-1-enecarboxylate phosphate, from (-)-shikimic acid was studied. The main parameters of ...
