DERIVATIVES OF PHOSPHONESUCCINIC ACID AND THEIR PHARMACOLOGICALLY ACCEPTABLE SALTS AND COMPOSITION BASED ON THEREOF Russian patent published in 1998 - IPC

FIELD: organic chemistry, organophosphorus compounds. SUBSTANCE: products: derivatives of phosphonesuccinic acid of the formula R-alk-CH(CO₂R⁴)-CH(CO₂R³P(O)(OR⁵)₂ where R - amino-group, NR₁R₂; R₁ and R₂ - H, C₁-C₆-alkyl; nitrogen-containing five-membered heterocyclic ring is taken from the group involving phthaloylimide, imidazole, pyrrolidine; alk - covalent bond, methylene or alkylene containing 2-6 carbon atoms; R³, R⁴ and R⁵ - H, C₁-C₆-alkyl and their pharmacologically acceptable salts. When R³, R⁴ and R⁵ mean methyl and alk means covalent bond then R can not mean dimethylamino-group. Reagent 1: derivative of carboxylic acid of the formula R-alk-CH(Y)-CO₂R⁴ where R, alk and R⁴ have the above indicated values; Y - splitting off group. Reagent 2: compound of the formula H₂C(CO₂R³)P(O)(OR⁵)₂ where R³ and R⁵ have the above indicated values. Reaction conditions: in medium of organic solvent, in the presence of base. Synthesized compounds are used in medicine for treatment of calcium metabolism disorders. EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 3 cl, 2 tbl, 10 ex