NOVEL BUTYROPHENONE DERIVATIVE

NEW MATERIAL:A butyrophenone derivative shown by the formula I (Ar is phenyl group with is replaced with 1-2 lower alkoxy group or alkylenedioxy group) or its acid addition salt. EXAMPLE:gamma-(4-Phenylpiperidino)-3,4-dimethoxybutyrophenone hydrochloride. USE:Having Ca antagonism, antihypertensive a...

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Hauptverfasser: SAITOU KUNIAKI, KOJO KENTARO, MASUKO TOSHIHISA
Format: Patent
Sprache:eng
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Zusammenfassung:NEW MATERIAL:A butyrophenone derivative shown by the formula I (Ar is phenyl group with is replaced with 1-2 lower alkoxy group or alkylenedioxy group) or its acid addition salt. EXAMPLE:gamma-(4-Phenylpiperidino)-3,4-dimethoxybutyrophenone hydrochloride. USE:Having Ca antagonism, antihypertensive action, useful as a drug for circulatory system. PREPARATION:A gamma-arylbutyryl halide derivative shown by the formula II (X is halogen) is reacted with 4-phenylpiperidine in the absence of a solvent or in a solvent such as an alcohol, benzene, etc. in the presence of a base such as preferably triethylamine, potassium carbonate, etc. at room temperature - the boiling point of the solvent for 30min-1hr to give a compound shown by the formula I. When this compound is converted into an acid addition salt, hydrochloric acid, phthalic acid, etc. is used as the acid.