3-CARBALKOXYAMINO-5-(α-AMINOPROPIONYL) -5H-DIBENZ-[B,F] -AZEP-INES SHOWING ANTIARRHYTMIC ACTIVITY Russian patent published in 1995 - IPC

FIELD: heterocyclic compounds. SUBSTANCE: product: 3-carbalkoxyamino-5- (a-aminopropionyl) -5H-[b,f]-azepines of the general formula (I) where at X - -(CH₂)₂- a) R₁= R₂= CH₃ R₃ - H, n= 1; b) R₁= CH₃ R₂= C₂H₅OH n=1; c) R₁= C₂H₅ R₂= R₃= CH₃ n=1; d) R₁= C₂H₅ R₂= CH₃, R₃= H n=0 or 1; e) R₁= R₂= C₂H₅ R₃ - H, n=1; f) R₁= C₂H₅ R₂= H-C₃H₇ R₃ - H, n=1; g) R₁= C₂H₅ R₂= R₃= CH₃ n=1; h) R₁≠ R₂= R₃= C₂H₅, n=1; i) R₁= C₂H₅ (R₂+R₃) = -(CH₂)₂-O-(CH₂)₂- n= 1; j) R₁= ISO-C₃H₇ R₂= CH₃ R₃ - H, n=0; k) R₁-изо-C₃H₇ R₂= C₂H₅, R₃= H n=1; at X - -CH=CH- l) R₁= C₂H₅, R₂= CH₃, R₃= H n= 0; m) R₁= R₂= C₂H₅, R₃= H n=1. Synthesis is carried out by reaction of 3-carbalkoxyamino-10,11-dihydro- 5H-dibenz-[b,f]-azepine with α-chloropropionyl chloride in the medium of inert solvent (benzene) in the presence of HCl acceptor (pyridine) at the boiling of reaction mass. Then product is treated with corresponding amine: NHR₂R₃ in the medium of solvent at the boiling. Synthesized compounds show antiarrhytmic activity, their activity exceeds that of bonnecor with decreased toxicity. EFFECT: synthesis of new compounds of class indicated above showing enhanced activity and lowered toxicity. 1 tbl