Синтез и свойства 2-замещенных амидов цинхониновой кислоты

Novel substituted 2-clorcinchoninic acid amides were synthesized by reaction of acid 2-clorcinchoninic acid with alkylor arylamines. Heating of substituted 2-clorcinchoninic acid amides in acetic acid in the presence of sodium acetate (method A) leads to the corresponding amides of 1,2-dihydro-1H-2oxocinchoninic acid. Heat-ing of ethyl ester of 1,2-dihydro-1H-2-oxocinchoninic acid with an alkyl or arylamines in ethylene glycol also leads to the formation of 1,2-dihydro-1H-2-oxocinchoninic acid amides (method B). The structure of synthesized compounds was confirmed by spectral methods. Biological trials have revealed that 1,2-dihydro-1H-2-oxocinchoninic acid allilamide and hexadecylamide 1,2-dihydro-1H-2-oxocinchoninic acid have anti-inflammatory and analgetic activity. Diclofenac sodium (orthofen), acetylsalicylic acid (aspirin) and metamizole sodium (analgin) have been used as reference substances. Further search of biologically active compounds in this series is promising.