RACEMIC OR OPTICALLY ACTIVE DERIVATIVES OF PYRIDO[1,2-A]PYRAZINE Russian patent published in 1994 - IPC

FIELD: organic chemistry. SUBSTANCE: products - racemic or optically active derivatives of pyrido[1,2-a]pyrazine of the general formula I, where X - N or CH; Y - a) ; b) ; c) ; d) ; Z - a) ; b) , SH₂, OCH₂, Y¹(CH₂)_n; n = 1 or 2; Y¹-CH₂, NH or NCH₃; yield is 30-40%. Products - racemic derivatives of pyrido[1,2-a] pyrazine of the general formula II, where at A - H, B = C₁-C₃-alkoxycarbonyl, X¹ - carbonyl; at A - H or group , X - N or CH; X¹-CH₂, B - CH₂OH; at A - group , X - N or CH; X¹-CH₂, B - Y²CH₂-,Y² - OH; RSO₂O, NH₂-, N₃ or ; R - C₁-C₃-alkyl, phenyl, tolyl. Products - optically active derivatives of pyrido[1,2-a] pyrazine of the general formula III, where X - N or CH; Y³ - OH; RSO₂O, R¹C(O)O or NH₂, R - C₁-C₃-alkyl, phenyl, tolyl; R¹ - C₁-C₃-alkyl. Reagent 1: compound of the general formula IV. Reagent 2: salt MY, where X and Y as indicated above for compound of the general formula I, M - alkaline metal. Reaction condition: in the medium of aprotonic polar solvent, at 90-120 C. Synthesized compounds are used in medicine as antidepressants and anxiolytics. EFFECT: improved method of synthesis. 4 cl