| 摘要 |
FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to alkyl derivatives of trazodone of the general formula (I) <EMI ID=0.487 HE=36 WI=60 TI=CHI> where only one of R, R', R' and R''' means C<SB>1-3</SB>-alkyl and others are hydrogen, and their salts with physiologically acceptable an inorganic or an organic acids. Compounds are synthesized by interaction of compound of the formula (III) <EMI ID=0.488 HE=27 WI=33 TI=CHI> or its alkaline metal salt with piperazine compound of the formula (II) <EMI ID=0.489 HE=21 WI=63 TI=CHI> where R, R', R'' and R''' have values as indicated in the formula (I) and X means chlorine or bromine at boiling point or reaction mass. Compounds of the formula (I) show decreased affinity to adrenergic receptors as compared with trazodone but exceeds trazodone with respect to value LD<SB>50</SB>. EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 10 cl, 8 ex
|
