2

Тhe technology basis of diclofenac substance production

The basis of the production technology of the diclofenac substance, which consists of five main technological stages, is justified and proposed. The proposed technological aspects of diclofenac substance production allow obtaining the target product with a total yield of 61%. Material calculations were carried out to obtain 1 ton of the final diclofenac substance. The numbers of necessary technological equipment are selected, and a basic technological scheme for the production of diclofenac is proposed.

THERMODYNAMIC PROPERTIES OF METHYL ESTER OF 6-METHYL-2-OXO-4-ARYL-1,2,3,4- TETRAHIDROPIRYMIDYN-5-CARBOXYLATE IN ETHYLACETATE AND BENZENE AND THEIR MIXTURE

The purpose of this work is to investigate the thermodynamic properties of the solubility of methyl 6-methyl-2-oxo-4-phenyl-1,2,3,4-tetrahydro-pyrimidine-5-carboxylate, which exhibits a wide spectrum of biological activity in organic solvents of different polarity and their character of mixing. As you know, the processes of synthesis and purification of solid substances, allmost, occur with the help of individual solvents or their mixture, so optimization of these processes is impossible without determining the thermodynamic parameters of their dissolution.

One-Pot Synthesis, Antioxidant Activity and Toxicity Evaluation of Some Hydroxyxanthones

Some new hydroxyxanthone compounds were prepared through one pot cyclodehydration reaction of hydroxybenzoic acid derivatives (salicylic acid or resorcylic acid) with phloroglucinol or pyrogallol in the presence of Eaton’s reagent (P2O5/MeSO3H). The synthesized compounds were screened for their antioxidant activities by 2,2-diphenyl-1-picrylhydrazyl (DPPH) methods to determine their inhibitory concentration (IC50). Cytotoxicity of the prepared compounds was also evaluated by MMT assay on Vero cell line.

SYNTHESIS OF TIOSOLFOESTERS WITH S-TRIAZINE FRAGMENT

Cyanuric chloride is a valuable starting agent for the direct obtaining of highly structured molecules. The substitution of chlorine atoms in the molecule of cyanuric chloride by various pharmacophores’ fragments provides the obtaining a number of 1,3,5-triazine derivatives, among which the promising biologically active substances showing antimicrobial, anticancer, antimalarial and antiviral activity were detected.

THERMODYNAMIC PROPERTIES OF THE SOLUBILITY OF ESTERS OF 6-METHYL-2-OXO-4-ARYL-1,2,3,4-TETRAHIDROPIRYMIDYN-5- CARBOXYLIC ACID IN ACETONITRILE

The derivatives of 6-methyl-2-oxo-4-phenyl-1,2,3,4-tetrahydropyrimidine-5-carboxylic acid are the simplest representatives of Bidzhenelli’s dyhidropirymidynes and are characterized by a wide range of biological activity. It is important to use pure substances at each stage of the synthesis in the pharmaceutical industry. The main method of solid substances purifying is recrystallization using the so-called "classic" solvents, which include acetonitrile.

Тіопіранотіазолонові похідні просторово екранованого фенолу

Просторово екранований фенол входить в структуру дарбуфелону - відомого нестероїдного протизапального засобу. Одержано тіопіранотіазолонові похідні із застосуванням гетеро-варіанту реакції Дільса-Альдера в ацетатній кислоті взаємодією 5-(3,5-ди-трет-бутил-4-гідроксибензиліден)-4-тіокси-2-тіазолідону з феніл-пірол-2,5-діоном, 1-п-толіл-пірол-2,5-діоном, 1-(4-метокси-феніл)пірол-2,5-діоном і пропеналем. Підтверджено будову синтезованих сполук та наведено їх спектральні характеристики.

Термодинамічні властивості розчинів метил 6-метил-2-оксо-4-феніл- 1,2,3,4-тетрагідропіримідин-5-карбоксилату в органічних розчинниках

За температурною залежністю розчинності метилового естеру 6-метил-2-оксо-4-арил-1,2,3,4-тетрагідропіримідин-5-карбонової кислоти в ізопропанолі, етилацетаті та бензолі розраховано ентальпію та ентропію його розчинення. З врахуванням ентальпії плавлення, визначеної за даними диференційно-термічного аналізу та перерахованої на 298К, розраховано ентальпії та ентропії змішування за 298 К. Показано вплив розчинника на розчинність та величини ентальпії і ентропії змішування при 298К.

Obtaining of coumarone-indene resins based on light fraction of coal tar 1. coumarone-indene resins with carboxy groups

Coumarone-indene resins (CIR) with carboxy groups were synthesized via cooligomerization of unsaturated compounds presented in light fraction of coal tar and its fraction boiling out within 423–463 K with the addition of such industrial monomers as styrene, maleic anhydride, glycidyl methacrylate and methacrylic acid. 2,2`-Azobis(2-methylpropionitrile) in the form of 0.2 M solution in toluene was used as an initiator. The effect of monomers nature, initiator amount, temperature and reaction time on the yield and characteristics of resulted CIR has been determined.

Дослідження кінетичних закономірностей димеризації 2,3-диметилбута-1,3-дієну

Kinetic regularities of 2,3-dimethyl-buta-1,3-diene dimerization as a second-order reaction taking place in two parallel directions have been researched. Experimental kinetic data were obtained by gas chromatography. The activation parameters obtained for 2,3 dimethyl-buta-1,3-diene dimerization indicate that the reaction takes place in the kinetic region. Досліджено кінетичні закономірності димеризації 2,3-диметилбута-1,3-дієну як реакції другого порядку, яка відбувається за двома паралельними напрямками. Експериментальні кінетичні дані були отримані методом газохроматографічного аналізу.

Alkylation of 2,6-di-tert-Butylphenol with Methyl Acrylate Catalyzed by Potassium 2,6-di-tert-Butylphenoxide

The kinetics of catalytic alkylation of 2,6-di-tert-butylphenol (ArOH) with methyl acrylate (MA) in the presence of potassium 2,6-di-tert-butylphenoxide (ArOK) depends on the method for the preparation of ArOK. The reaction of ArOH with KOH at temperatures > 453 K affords monomeric ArOK, which properties differ from those in the case of potassium 2,6-di-tert-butylphenoxide synthesized by the earlier methods. The regularities of ArOH alkylation depend on the ArOK concentration, the ArOH:MA ratio, and the effect of microadditives of polar solvents.