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5-Aryl-4-(4-halobenzoyl)-3-hydroxy-1-carboxymethyl-3-pyrrolin-2-ones were obtained by a three-component reaction of methyl esters of p-halobenzoylpyruvic acids with a mixture of aromatic aldehyde and glycine in glacial acetic acid in the presence of anhydrous sodium acetate. The analgesic activity of the obtained compounds was studied using the hot-plate method. Their anti-inflammatory activity was determined using the aseptic carrageenan inflammation model. It was shown that all compounds under study exhibit pronounced analgesic activity while compound III also had pronounced anti-exudative activity. [ABSTRACT FROM AUTHOR]

Three-component Biginelli reaction of ethyl 4-(2,4-dioxo-4-phenylbutanamido)benzoate, aromatic aldehyde and thiourea in acetic acid in the presence of sodium acetate led to the formation of ethyl 4-(6-aryl-5-benzoyl-4-hydroxy-2-thioxohexahydropyrimidine-4-carboxamido)benzoates. Structure of the obtained compounds was established by IR, 1H NMR, 13C spectroscopy methods. [ABSTRACT FROM AUTHOR]

The reaction of methyl esters of 4-aryl-2-hydroxy-4-oxobut-2-enoic acids (aroylpyruvic acids) with 4-aminobenzoic acid ethyl ester (benzocaine, anesthesin) in glacial acetic acid in the presence of anhydrous sodium acetate gave rise to ethyl (Z)-4-(4-aryl-2-hydroxy-4-oxobut-2-enamido)benzoates. Analgesic activity of the synthesized compounds was studied. [ABSTRACT FROM AUTHOR]

The reaction of methyl esters of aroylpyruvic acids with methyl 2-aminobenzoate in glacial acetic acid in the presence of anhydrous sodium acetate afforded a series of methyl 2-{[(2Z)-4-aryl-2-hydroxy-4-oxobut-2-enoyl]amino}benzoates. The analgesic activity of the synthesized compounds was studied. [ABSTRACT FROM AUTHOR]

A series of 5-aryl-4-acetyl-3-hydroxy-1-carboxymethyl-3-pyrrolin-2-ones were synthesized by reacting acetylpyruvic acid methyl ester with a mixture of an aromatic aldehyde and glycine in glacial acetic acid and distilled water. The analgesic activity of the obtained compounds was studied using the hot-plate test. Their anti-inflammatory activity was determined using the model of aseptic carrageenan-induced inflammation. It was found that the synthesized compounds had pronounced analgesic activity and belonged to low-toxicity substances. [ABSTRACT FROM AUTHOR]

Reaction of 2,4-diamino-6-hydroxypyrimidine with methyl 4-aryl-2,4-dioxobutanoates in acetic acid led to the formation of methyl 2-amino-7-aryl-4-oxo-3H-pyrido[2,3-d]pyrimidine-5-carboxilates. Structure of the obtained compounds was confirmed by single crystal X-ray analysis. [ABSTRACT FROM AUTHOR]

The reaction of (4-chlorobenzoyl)pyruvic acid methyl ester with a mixture of aromatic aldehyde and 4-aminobenzoic acid ethyl ester in glacial acetic acid afforded ethyl 4-[5-aryl-3-hydroxy-2-oxo-4-(4-chlorobenzoyl)-2,5-dihydro-1H-pyrrol-1-yl]benzoates. [ABSTRACT FROM AUTHOR]

A series of new 1-aminocarbonylmethyl-5-aryl-4-aroyl-3-hydroxy-3-pyrrolin-2-ones has been synthesized through a three-component reaction of aroylpyruvic acid methyl ester with a mixture of aromatic aldehyde and glycinamide hydrochloride in glacial acetic acid in the presence of anhydrous sodium bicarbonate. [ABSTRACT FROM AUTHOR]

5-Aryl-4-aroyl-3-hydroxy-1-cyanomethyl-3-pyrrolin-2-ones were synthesized by a three-component reaction of aroylpyruvic acid methyl ester with a mixture of aromatic aldehyde and 2-aminoacetonitrile sulfate in glacial acetic acid in the presence of anhydrous sodium acetate. The possibility of their reactions with p-toluidine and hydrazine hydrate was shown. [ABSTRACT FROM AUTHOR]

Reactions of 5-aryl-4-aroyl-3-hydroxy-1-cyanomethyl-3-pyrrolin-2-ones with aromatic amines in glacial acetic acid afforded 5-aryl-3-arylamino-4-aroyl-1-cyanomethyl-3-pyrrolin-2-ones and 5-aryl-4-[aryl(arylamino)-methylene]-1-cyanomethyltetrahydropyrrole-2,3-diones. In the case of 5-aryl-4-acetyl-3-hydroxy-1-cyanomethyl-3-pyrrolin-2-ones the reactions led to the formation of 5-aryl-4-(1-arylaminomethylene)-1-cyanomethyltetrahy-dropyrrole-2,3-dione. [ABSTRACT FROM AUTHOR]

Three-component reaction of methyl 4-aryl-2,4-dioxobutanoates with aromatic aldehyde and 2-aminoacetonitrile sulfate in glacial acetic acid in the presence of anhydrous sodium acetate afforded previously unknown (3-aroyl-2-aryl-4-hydroxy-5-oxo-2,5-dihydro-1H-pyrrol-1-yl)acetonitriles. The reaction involved intermediate formation of Schiff base, followed by Michael-type addition of the dioxo ester to the C=N bond and cyclization of the addition product, methyl 3-aroyl-4-aryl-4-(cyanomethylamino)-2-oxobutanoate. The cyclization product reacted with hydrazine hydrate at the aroyl carbonyl group to give the corresponding hydrazone which was converted in 1,4-dioxane to the cyclic form, [3,4-diaryl-6a-hydroxy-6-oxo-3a,4,6,6a-tetrahydropyrrolo[3,4-c]pyrazol-5(1H)-yl]acetonitrile, without elimination of the second water molecule. When the reaction of (3-aroyl-2-aryl-4-hydroxy-5-oxo-2,5-dihydro-1H-pyrrol-1-yl)acetomtriles with hydrazine hydrate was carried out in boiling acetic acid, [3,4-diaryl-6-oxo-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]acetonitriles were obtained as a result of dehydration of initially formed [3,4-diaryl-6a-hydroxy-6-oxo-3a,4,6,6a-tetrahydropyrrolo[3,4-c]pyrazol-5(1H)-yl]acetonitriles as shown by special experiment. The structures of [6a-hydroxy-6-oxo-3,4-diphenyl-3a,4,6,6a-tetrahydropyrrolo[3,4-c]pyrazol-5(1H)-yl]acetonitrile and [4-(4-methoxyphenyl)-6-oxo-3-phenyl-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]acetonitrile were determined by X-ray analysis. [ABSTRACT FROM AUTHOR]

The reaction of methyl aroylpyruvates with 2-(4-aminobenzenesulfonamido)thiazole (norsulfazole) in acetic acid-ethanol (1: 1) afforded methyl (2Z)-4-aryl-4-oxo-2-{4-[(1,3-thiazol-2-yl)sulfamoyl]phenyl-amino} but-2-enoates which reacted with ninhydrin in glacial acetic acid to give 4-aroyl-3-{4-[(1,3-thiazol-2-yl)-sulfamoyl]phenylamino} spiro[2,5-dihydrofuran-5,2′-indane]-2,1′,3′-triones. [ABSTRACT FROM AUTHOR]

The reaction of methyl aroylpyruvates and 2-(4-aminobenzenesulfamido)-4,6-dimethylpyrimidine in glacial acetic acid in the presence of anhydrous sodium acetate afforded (2Z)-4-aryl-2-hydroxy-N-{4-[(4,6-dimethylpyrimidin-2-yl)sulfamoyl]phenyl}-4-oxobut-2-enamides. Reaction of the above reagents in a mixture of acetic acid and ethanol (1: 1) in the absence of anhydrous sodium acetate gave methyl (2Z)-4-aryl-2-{4-[(4,6-dimethylpyrimidin-2-yl)sulfamoyl]phenylamino}-4-oxobut-2-enoates. Analgesic and anti-inflammatory activities of the synthesized compounds was studied. [ABSTRACT FROM AUTHOR]

5-Aryl-4-aroyl-3-hydroxy-1-cyanomethyl-3-pyrrolin-2-ones were synthesized by a three-component reaction of methyl aroylpyruvate with a mixture of aromatic aldehyde and 2-aminoacetonitrile sulfate in glacial acetic acid in the presence of anhydrous sodium acetate. [ABSTRACT FROM AUTHOR]

Reactions of 5-phenyl-2,3-dihydrofuran-2,3-dione with aromatic amines in anhydrous dioxane or methyl benzoylpyruvate with aromatic amines in the presence of sodium acetate in glacial acetic acid afforded (Z)-N-aryl-2-hydroxy-4-oxo-4-phenylbut-2-enamides. [ABSTRACT FROM AUTHOR]

The reaction of methyl aroylpyruvates with 2-(4-aminobenzenesulfamido)thiazole (norsulfazole) in glacial acetic acid in the presence of anhydrous sodium acetate furnished 4-aryl-2-hydroxy-4-oxo-N-{4-[(1,3-thiazol-2-yl)sulfamoyl]phenyl}but-2-eneamides. [ABSTRACT FROM AUTHOR]

The reaction of methyl 4-aryl-2,4-dioxobut-2-enoates with 4-aminobenzenesulfonamide in acetic acid-ethanol (1: 1) afforded methyl (2 Z)-4-aryl-4-oxo-2-(4-sulfamoylanilino)but-2-enoates which reacted with ninhydrin in glacial acetic acid to give 3-aroyl-4-(4-sulfamoylanilino]-5 H-spiro[furan-2,2′-indene]-1′,3′,5-triones. [ABSTRACT FROM AUTHOR]

Baeyer-Villiger oxidation of N, N,2-triaryl-6-hydroxy-6-methyl-4-oxocyclohexane-1,3-dicarboxamides with 30% hydrogen peroxide in acetic acid afforded 2-(4-aryl-3-carbamoyl-2-methyl-5-oxooxolan-2-yl)acetic acids. [ABSTRACT FROM AUTHOR]

Reaction of methyl aroylpyruvates with 4-aminobenzolsulfonylguanidine in acetic acid in the presence of anhydrous sodium acetate afforded N-(4-guanidylsulfonylphenyl)amides of 4-aryl-2-hydroxy-4-oxo-2-butenoic acids. Antibacterial activity of the synthesized compounds was studied. [ABSTRACT FROM AUTHOR]

Alkyl 5-aryl-7-methyl-1,5-dihydrotetrazolo[1,5- a]pyrimidine-6-carboxylates were obtained by melting acetoacetic acid esters with 5-aminotetrazole and aromatic aldehyde. [ABSTRACT FROM AUTHOR]

The article discusses research that described the synthesis and antimicrobial activity of novel pyrrolo[3,4-c]pyrazol-6-one derivatives. Topics covered include reactions of 1-[2-(4-aminosulfonyl-phenyl)ethyl]-5-aryl-4-aroyl-3-hydroxy-3-pyrrolin-2-ones with hydrazine hydrate, glacial acetic acid under reflux, and production of 5-[2-(4-aminosulfonyl-phenyl)ethyl]-3,4-diaryl-4,6-dihadropyrrolo[3,4-c]pyrazol-6-ones.

6-Acyl-7-aryl-4,7-dihydrotetrazolo[1,5- a]pyrimidine-5-carboxylic acids and methyl 6-acyl-7-aryl-4,7-dihydrotetrazolo[1,5- a]pyrimidine-5-carboxylates were synthesized by fusion of 4-aryl-2,4-dioxobutanoic acids and their methyl esters, respectively, with 1 H-tetrazol-5-amine and aromatic aldehydes. The reaction of methyl 2,4-dioxopentanoate with 1 H-tetrazol-5-amine and 2-fluorobenzaldehyde in boiling acetic acid gave methyl 6-acetyl-5-hydroxy-7-(2-fluorophenyl)-4,5,6,7-tetrahydrotetrazolo[1,5- a]pyrimidine-5-carboxylate. [ABSTRACT FROM AUTHOR]

Ethyl 6-amino-4-aryl-5-cyano-1,4-dihydropyrano[2,3- c]pyrazol-3-carboxylates were synthesized by a reaction of diethyloxalacetate sodium salt with aromatic aldehyde, hydrazine hydrate, and malononitrile in the presence of acetic acid. [ABSTRACT FROM AUTHOR]

The article focuses on the synthesis of 2-aroylmethylidine-6-hydroxy-2,3-dihydroindol-3-ones which is an end-product of the reaction of methyl 4-aryl-2,4-dioxobutanoates with 3-amino-phenol in boiling acetic acid. Methyl 4-aryl-2-arylamino-4-oxobut-2-enoates are derived from the reaction of methyl 4-aryl-2,4-dioxobutanoates with aromatic amines. However, the reaction was noted to produce almost no by-products regardless of the substituent in the aromatic amine and solvent nature.

The article provides information about the synthesis of Methyl 6-Acyl-7-aryl-4,7-dihydrotetrazolo- pyrimidine-5-carboxylates. It reports that researchers have found that fusion of methyl acylpyruvates with 5-aminotetrazole and aromatic aldehydes at 120-150 degree Celsius gives methyl 6-acyl-7-aryl-4,7-dihydrotetrazolo pyrimidine-5-carboxylates I-III Compounds I-III are colorless crystalline substances readily soluble in DMSO and DMF, soluble in hot alcohol, acetic acid, and dioxane, and insoluble in water.