Pyridopyrrolobenzheterocycles

Details Pyridopyrrolobenzheterocycles Pyridopyrrolobenzheterocycles

1976-12-28

1978-09-19

Rotman, Alan L.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Bacterium or component thereof or substance produced by said...

544 14, 544 99, 2602948A, C07D49522, A61K 3144

Patent

active

041155777

ABSTRACT:
##STR1## where X is 0, S, S.fwdarw.O, or SO.sub.2 ; n is O 0 1; m is 0 or 1; the R's are the same or different and are H or CH.sub.3, and one of them can be C.sub.2 -C.sub.9 alkyl, phenyl, C.sub.7 -C.sub.10 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 OCH.sub.3 ; when X is S and m is 1, the R in the group (CHR).sub.m can be OCH.sub.3 ; and R.sup.1 is H, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.2 -C.sub.4 alkoxycarbonyl, trifluoroacetyl, or substituted C.sub.1 -C.sub.4 alkyl where the substituent is C.sub.3 -C.sub.6 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 ##STR2## wherein R.sup.2 is R.sup.1 or acyl. The latter compounds are prepared by reacting 4-piperidones with compoounds of formula III in the presence of a reducing agent ##STR3## or with compounds of formula VI ##STR4##

REFERENCES:
patent: 3401166 (1968-09-01), Krapcho
patent: 3914421 (1975-10-01), Rajagopalan

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