INDOLE DERIVATIVES, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION Russian patent published in 1999 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to derivative of indole of the general formula (I): or its physiologically acceptable salt, or metabolically labile ester where R means chlorine atom at position 4 and 6 of indole ring; R₂ means phenyl possibly substituted with one or two groups taken from fluorine atom, trifluoromethyl-group, lower alkyl and alkoxy-, hydroxy- and nitro-groups; X means NH. Methods of synthesis of indicated derivatives involve an interaction of the corresponding indole containing a carboxy-protective group and a group CR₄O where R₄ - hydrogen atom or C₁-C₄-alkyl with phosphorus ylide of the formula: (R₅)₃P=CH-COXR₂ or (R₇O)₂OP=CR₆-COXR₂ where R₅ - alkyl or phenyl; R₆ - hydrogen atom or C₁-C₄-alkyl; R₇ is C₁-C₄-alkyl and X and R₂ are indicated above. Synthesized derivatives of indole are active components of a pharmaceutical composition. Composition shows properties of antagonist of amino acids exciting NMDA-receptor complex. EFFECT: improved method of synthesis, antagonistic properties of a composition with respect to some amino acids. 13 cl, 2 tbl, 12 ex