5-(ω-AMINOACYL)-5,10-DIHYDRO-11H-DIBENZO-[B,E][1,4] -DIAZEPI- NE-11-ONES OR THEIR SALTS SHOWING ANTIARRHYRMIC ACTIVITY Russian patent published in 1995 - IPC

FIELD: heterocyclic compounds. SUBSTANCE: product: 5-(w-aminoacyl)-5,10-dihydro-11H-dibenzo-[b, e] [1,4] -diazepi- ne-11-ones of the general formula (I) where 1) R₁ - H, R₂= R₃= CH₃ n=5, X - Cl, m=1; 2) R₁ - H, R₂= R₃= C₂H₅ n=3 or 5, m=0; 3) R₁ - H, R₂= R₃= C₂H₅ n=5, m=1, X - Cl; 4) R₁ - Cl, R₂= R₃= C₂H₅ n=3-6, m=0; 5) R₁ - Cl, n=5 or 6, m=0; 6) R₁ - Cl, n=5, m=0; 7) R₁ - Cl, H; R₂ - H, R₃= C₂H₅; n=5, X - Cl, m=1 8) R₁ - Cl, R₂ - H, n=5, m=1, X - Cl; 9) R₁ - H; , n=5, m=1, X - Cl; 10) R₁= R₂ - H; , n=5, m=1, X - Br; 11) R₁ - H, R₂= R₃= -CH(CH₃)₂, n=5, m=0; 12) R₁ - Cl, n= 3, m=0. Synthesis is carried out, for example, by reaction of corresponding diazepinone-11 with dialkylamine in dimethylformamide medium at 2 C following by slowly heating up to 30 C, solvent distillation off, treatment with solution of NH₃ and CHCl₃, extraction with HCl (1:1), alkalinization of acid phase, extraction with CHCl₃, its distillation off, mixing with acetone, passing of HCl up to pH=1, evaporation, mixing with ethylacetate and acetone and recrystallization from isopropanol. Synthesized compounds show antiarrhytmic activity, their toxicity is two-fold less than lidocaines (LD₅₀= 28-144 mg/kg against 18 mg/kg) with increased activity (therapeutical range is 12-1810 against 5.8) and can be used in medicine. EFFECT: synthesis of new compounds of class indicated above. 1 tbl