Tsapko T. Synthesis, physico-chemical properties and biological activity of sulfoderivatives of 4-methyl-1,2-dihydroquinolin-2-ones

Study of sulfochlorination of 4-methyl-1,2-dihydroquinolin-2-one derivatives with substituents in benzoic ring has been done for the first time. In order to find new biologically active substances рreparative methods for obtaining of 4-methyl-2-oxo-1,2-dihydroquinolin-6-sulfonylamides, 6-alkylsulfonyl-4-methyl-1,2-dihydroquinolin-2-ones and 4 methyl-2-oxo-1,2-dihydroquinolin-6-sulfonylacetic acid amides have been developed and wide series of these compounds have been synthesized. Alkylation of 4-methyl-2-оxо-1,2-dihydroquinolin-6-sulfinic acid with allylbromide has been investigated. It has been found that the product of this reaction, depending on conditions, is the corresponded allylsulfone or its mixture with isomeric propenylsulfone. Antimicrobial, diuretic, haemostatic and anticoagulant activity of new compounds has been studied, some structure-activity relationships have been revealed. As a result, 4 methyl-7-chloro-2-оxо-1,2-dihydroquinolin-6-sulfonic acid n-butylamide, which has potent diuretic activity, has been proposed for profound biological research.