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
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Authors
Dates
1995-01-20—Published
1989-11-29—Filed