| 摘要 |
Title comds. I (R,R1 = H, C1-3 alkyl, C1-3 cycloalkyl, c1-8 aralkyl; X, Y = Cl, Br, F, C1-3 alkyl, OH, CF3; m = 0-1, n = 0-3, integer) and their physiol. acceptable salts. useful as antidepressants, analgesics, and anticonvulsants were prepd. 2-(O2N)C6H4CH2COPh was successively oximated(H2NOH), acylated, reduced(diborane), alkalized(NaOMe) and hydrogenated to give 2-H2NC6H4CH2CH(NH2)PHHCl which was cyclized with HC(OEt), in refluxing EtOH-HCl to give I (X-Y = H)HCl. I(X-Y = H)HCl had antidepressant ED50 20 mg/kg (mice) i.p., analgesic ED50 21.3 mg/kg (mice) s.c., and anticonvulsant ED50 19.4 mg/kg (mamma/s) i.p.
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