摘要 |
<IMAGE> I where X is O, S, S->O, or SO2; n is 0 or 1; m is 0 or 1; the R's are the same or different and are H or CH3, and one of them can be C2-C9 alkyl, phenyl, C7-C10 phenylalkyl, furyl, thienyl, pyridyl or substituted phenyl or phenylalkyl; when X is S, and m is 0, one R in the group -RCR- can be OCH3; when X is S and m is 1, the R in the group (CHR)m can be OCH3; and R1 is H, C1-C4 alkyl, C3-C5 alkenyl, C3-C5 alkynyl, C3-C6 cycloalkyl, C2-C4 alkoxycarbonyl, trifluoroacetyl, or substituted C1-C4 alkyl where the substituent is C3-C6 cycloalkyl, phenyl or substituted phenyl; and their pharmaceutically suitable salts. The compounds are useful as sedatives; some of them also exhibit antidepressant, antihypertensive and antibacterial activity. The compounds are prepared by cyclizing compounds of formula II <IMAGE> II wherein R2 is R1 or acyl. The latter compounds are prepared by reacting 4-piperidones with compounds of formula III in the presence of a reducing agent <IMAGE> III or with compounds of formula VI <IMAGE>VI
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