SUBSTITUTED CYCLOHEPTENE, ITS PRODUCTION AND USE

PROBLEM TO BE SOLVED: To provide a new substituted cycloheptene having biological effectiveness originated partially or mainly from δ-opiate receptor agonist and useful for analgesic use. SOLUTION: The objective substituted cycloheptene is expressed by formula I [R1 is OH, an O-(1-6C alkyl), an O-(3...

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Hauptverfasser: ZIMMER OSWALD DR, ENGLBERGER WERNER GUENTER DR, STRASBURGER WOLFGANG WERNER A, KOEGEL BABETTE-YVONNE DR
Format: Patent
Sprache:eng
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Zusammenfassung:PROBLEM TO BE SOLVED: To provide a new substituted cycloheptene having biological effectiveness originated partially or mainly from δ-opiate receptor agonist and useful for analgesic use. SOLUTION: The objective substituted cycloheptene is expressed by formula I [R1 is OH, an O-(1-6C alkyl), an O-(3-7C cycloalkyl), an O-aryl, a 1-6C alkyl- COO or the like; R2 is a 1-6C alkyl, a 2-6C alkenylene-aryl or the like; R3 is (CH2)0-1-(5-7C cycloalkyl), (CH2)0-2-aryl or the like], e.g. 3-[6-(4-chloro-phenyl)-2- dimethylaminomethyl-cyclo-hept-1-enyl]-phenol. The compound of formula I can be produced by reacting a t-alcohol of formula II with an acid at 20-110 deg.C. The compound of formula II can be produced by reacting an aminoketone of formula III (R4 is same as R3 and the like) with an organometallic compound of formula IV (X is MgCl or the like; R5 is same as R1 and the like).