abstract |
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 -CH 2 - or C(O); Z - phenyl, benzyl, α--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 - OSO 2 R′, CH-(Ar')-CH 2 Q″, CN where R' - -C 1 -C 4 -alkyl; Q'' - amino-group. EFFECT: improved method of synthesis. 11 cl |