PRODUCTION OF PYRROLOAZEPINE DERIVATIVE
PURPOSE:To economically synthesize a large amount of a pyrroazepine useful as an intermediate for a remedy for diseases of circulatory organs such as hypertension or heart-insufficiency from a readily obtainable pyrrole by a short process in excellent handleability. CONSTITUTION:Pyrrole shown by for...
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Zusammenfassung: | PURPOSE:To economically synthesize a large amount of a pyrroazepine useful as an intermediate for a remedy for diseases of circulatory organs such as hypertension or heart-insufficiency from a readily obtainable pyrrole by a short process in excellent handleability. CONSTITUTION:Pyrrole shown by formula III is reacted with a phosgene compound such as phosgene, trichloromethyl chloroformate or triphosgene and an amine derivative shown by formula IV (Y is COOR' or CN; R' is lower alkyl, aralkyl or aryl; R is H, alkyl or aralkyl) to give a pyrrolecarboxylic acid derivative shown by formula II by one-stage reaction. Then, optionally, this compound is hydrolyzed, then treated with a condensation agent selected from phosphorus pentoxide-methanesulfonic acid, phosphorus pentoxide- trifluoromethanesulfonic acid and methanesulfonic anhydride-methanesulfonic acid and subjected to ring formation to give the objective compound shown by formula I useful as an intermediate for a medicine having excellent anti-alpha1 action and antiserotonin action. |
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