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    • 53. 发明授权
    • Pyridopyrrolobenzheterocycles for combatting depression
    • 吡啶并吡唑并杂环用于对抗抑郁症
    • US3914421A
    • 1975-10-21
    • US35752873
    • 1973-05-07
    • ENDO LAB
    • RAJAGOPALAN PARTHASARATHI
    • C07D265/36C07D267/14C07D267/22C07D281/10C07D281/18C07D498/16C07D513/16A61K31/535
    • C07D267/14C07D265/36C07D267/22C07D281/10C07D281/18
    • 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)mcan be OCH3; and R1is 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

      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

      OR WITH COMPOUNDS OF FORMULA VI
    • 其中X是O,S.S-> O或SO2; n为0或1; m为0或1; 苯基,C7-C10苯基烷基,呋喃基,噻吩基,吡啶基或取代的苯基或苯基烷基;其中一个可以是C 2 -C 9烷基,苯基, 当X为S且m为0时,基团-RCR-中的一个R可为OCH 3; 当X为S且m为1时,基团(CHR)中的R可以是OCH 3; 和R 1为H,C 1 -C 4烷基,C 3 -C 5烯基,C 3 -C 5炔基,C 3 -C 6环烷基,C 2 -C 4烷氧基羰基,三氟乙酰基或取代的C 1 -C 4烷基,其中取代基为C 3 -C 6环烷基,苯基或取代苯基 ; 及其药学上合适的盐。 这些化合物可用作镇静剂; 其中一些还表现出抗抑郁,抗高血压和抗菌活性。