4-ALKYLENEPIPERIDINE DERIVATIVES OR THEIR SALTS WITH MINERAL OR ORGANIC ACIDS, OR QUATERNARY AMMONIUM SALTS SHOWING ACTIVITY WITH RESPECT TO NEUROKININ SYSTEM, A METHOD OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION

摘要

FIELD: organic chemistry. SUBSTANCE: products: derivatives of 4-alkylenepiperidine of the formula (I) given in description where Ar' - phenyl, naphthyl; R - H, methyl; Z' - phenyl, pyridyl; T' - simple bond or group -CH₂- or C(O); Z - phenyl, benzyl, --hydroxybenzyl, alkylphenyl, naphthyl; T - group C(O), or their salts. Reagent 1: compound of the formula (II) given in description where Pro-N - protective group which is subjected for catalytic hydrogenation in the presence of catalyst, for example, nickel Raney. The formed amine is subjected for interaction with acid HOCO-Z and the formed compound (after protection removal) is condensed with haloid derivative of the formula Z'-T'-Hal. Products: derivatives of 4-alkylenepiperidine of the formula (III) given in description where G - H, tert.-butoxycarbonyl or trityl; Q - OSO₂R, CH-(Ar')-CH₂Q, CN where R' - -C₁-C₄-alkyl; Q'' - amino-group. EFFECT: improved method of synthesis. 11 cl