2-BROMOELIMOCLAVINE HYDROBROMIDE SHOWING ADRENONEGATIVE EFFECT, ANTISEROTONINE ACTIVITY, NEUROTROPIC PROPERTIES AND INFLUENCE ON HEMODYNAMICS Russian patent published in 1994 - IPC

FIELD: organic chemistry. SUBSTANCE: for detection of activity of compounds of class indicated the compound I is synthesized. Synthesis is carried out from elimoclavine, triethylamine and N-bromosuccinimide in the medium of dioxane at 70 C for 2.5-3 h. Base I is a powder (color is from light-yellow to light-gray), m. p. is 229.5-231.5 C (with decomposition), R₁ = 0.22 (CHCl₃-CH₃OH-concentrated NH₃ = 90; 1: 1). I-hydrobromide is prepared by conventional method, decomposition point is 310-320 C. Adrenoblocking effect of I-hydrobromide is increased by 2-fold as compared with that of I-hydrochloride, but antiserotonine activity is similar. Effect of I-hydrobromide on peripheral vessels is 61.8% as compared 51.8% of that in I-chloride. I decreases frequency of heart beats, arterial blood pressure and increases blood flow in extremities. Toxicity of I: LD₅₀ = 53.5 and 268.9 mg/kg at intravenous and oral route of administration, respectively. EFFECT: enhanced pharmacological properties of drug. 2 tbl