PROCESS FOR PREPARING 2-AZAERYTHRINAN DERIVATIVES

The title compds. I [R1, R2, R3=H, alkoxy, halo, nitro, OH; Y=O, S, NH, NCH3, NCOC2H5, NCH2CH=CH2 -(CH2)m; m=0, 1; n=1, 2; R4=H alkyl, alkoxycarbonyl, -CH2CH=CR5R6;R5, R6=H, alkyl, ph; R7=H, halo, alkyl, alkoxy; R8=H, alkyl; R9=benzyl, penethyl, methyl, ethoxycarbonyl; R10=Et which exhibited analges...

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Hauptverfasser: MURAI HIROSI, MORIDA IWAO, ENOMODO HIROSI, MAZMURA SINGO, GIMURA GIYOSI, GAZNO KENGI
Format: Patent
Sprache:eng ; kor
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Zusammenfassung:The title compds. I [R1, R2, R3=H, alkoxy, halo, nitro, OH; Y=O, S, NH, NCH3, NCOC2H5, NCH2CH=CH2 -(CH2)m; m=0, 1; n=1, 2; R4=H alkyl, alkoxycarbonyl, -CH2CH=CR5R6;R5, R6=H, alkyl, ph; R7=H, halo, alkyl, alkoxy; R8=H, alkyl; R9=benzyl, penethyl, methyl, ethoxycarbonyl; R10=Et which exhibited analgesic activities, were prepd. Thus, ethy1-1-benzy1-4-piperidone-3-acetate, in anhyd. benzene was refluxed with ethylchloroformate for 2 hrs. to give ethyl-l-ethoxycarbony1-4-piperidone-3-acetate, which was refluxed again with β-penethylamine and toluene to give 2-benzyl-8-oxo-2-azaerythrinan.