| 摘要 |
<p>Substd. piperazine derivs. as spasmolytics, tranquillizers, psychostimulants; antibacterial and insecticidal agents; drug intermediates. Compds. of general formula I, their salts and quaternary salts are prepd. by conversion of compds. II to III and reaction of III with (a) R4OSO2R5, (b) Hal. COR7, (c) R6OCOR7, (d) halohydrin or alkylene carbonate, (e) R6Hal. (where A = C2-4-alkylene or alkylidene; R' = H, Ph or halophenyl; R" = lower alkyl, HO-alkyl, di-HO-alkyl, AlkO-alkyl, acyl, acyl-O-alkyl, or carbalkoxy; R3 = lower alkyl or benzyl; R4 = mono- or di-oxyalkyl; R5 = alkyl, Ph, totyl; R6 = lower alkyl; R7 = opt. Hal-substd. alkyl, Ph or (AlkO)3.Ph; m = 0-12; n = 4-7). Alternatively II may be replaced by IV and reacted with Hal.COR7 or R6Hal. or II may be reacted direct with R6Hal. When R3 = lower alkyl conversion of II to III is by strong alkali hydrolysis in alcoholic medium; when R3 = benzyl, by catalytic hydrogenation. I may be used as the separate stereoisomers or as the isomeric mixture.</p> |
