Ethyl ethers of 2-amino-1-benzoylamino-4-oxo-5- (2-oxo-2-arylethylidene) -4,5-dihydro-1H-pyrrolidine-3-carboxylic acids, which is beneficial in some respects.

摘要

1. Ethyl esters of 2-amino-1-benzoylamino-4-oxo-5- (2-oxo-2-arylethylidene) -4,5-dihydro-1H-pyrrolidine-3-carboxylic acids of the general formula Ia-ggde R - CHO (Ia), CHO (Ib), Br (Ic), Cl (Id), namely ethyl 2-amino-1-benzoylamino-4-oxo-5- [2- (4-methoxyphenyl) -2-oxoethylidene] -4,5-dihydro-1H-pyrrole-3-carboxylic acid (Ia), 2-amino-1-benzoylamino-4-oxo-5- [2- (4-ethoxyphenyl) -2-oxoethylidene] -4 ethyl ester , 5-dihydro-1H-pyrrole-3-carboxylic acid (IB), ethyl 2-amino-1-benzoylamino-4-oxo-5- [2- (4-bromophenyl) -2-oxoethylidene] -4.5 -dihydro-1H-pyrrole-3-carboxylic acid (Ic) and ethyl 2-amino-1-be nzoylamino-4-oxo-5- [2- (4-chlorophenyl) -2-oxoethylidene] -4,5-dihydro-1H-pyrrole-3-carboxylic acid (Ig), which exhibit antitumor activity. 2. The method of producing ethyl esters of 2-amino-1-benzoylamino-4-oxo-5- (2-oxo-2-arylethylidene) -4,5-dihydro-1H-pyrrolidine-3-carboxylic acids of the general formula Ia-d: where R - CHO (Ia), CHO (Ib), Br (Ib), Cl (Ig), which consists in the fact that 3-benzoylhydrazones 5-aryl-2,3-dihydro-2-furandiones (III) are reacted with cyanacetic ester in the presence of triethylamine in toluene for 20 minutes, and the precipitate formed is filtered off and recrystallized from a solvent mixture of benzene: ethanol (2: 1). 3. The use of a compound according to any one of paragraphs. 1-2 to obtain drugs for the treatment of cancer.