| 摘要 |
1412095 Dibenzo[a,d]cycloheptene derivatives RHONE-POULENC SA 28 Feb 1974 [2 March 1973 19 Oct 1973 23 Jan 1974] 9154/74 Heading C2C Novel compounds of the Formula I wherein X is hydrogen, halogen, alkyl, alkoxy, alkylthio, or trifluoromethyl; R 1 and R 2 , which are the same or different, each are hydrogen or alkyl and R 3 is hydroxy, alkoxy, 4-(2,2-dimethyl - 1,3 - dioxolanyl)methoxy or -NR 4 R 5 in which R 4 and R 5 which are the same or different, each are hydrogen, alkyl, hydroxyalkyl or phenyl or R 4 and R 5 together with the nitrogen to which they are attached are a mononuclear 5- or 6-membered heterocyclic ring optionally containing a second hetero atom selected from oxygen, sulphur and nitrogen which in the case of the second nitrogen atom is optionally substituted with alkyl, wherein all alkyl groups have 1 to 4 carbon atoms, and, when appropriate, salts thereof may be prepared (i) when R 3 is NH 2 , by cyclization and partial hydrolysis of a compound of the Formula II wherein Y is hydroxy or chlorine; (ii) when R 3 is OH, and salts thereof, by hydrolysis of a compound of the Formula V wherein T is cyano or carbamoyl, optionally followed by salt formation; (iii) wherein R 3 is as defined above other than hydroxy, by reaction of a compound R 3 -H with an acid halide (i.e. I in which R 3 is halogen) and optionally, where appropriate forming salts of the compounds I. Intermediates of the Formula II may be prepared by reacting an appropriate 4-(2-carboxy phenethyl)-chlorobenzene with an alkyl nitrile in sodamide. 2 - (5 - Oxo - 10,11 - dihydrodibenzo[a,d]cyclo hepten-2-yl propionyl chloride may be prepared by reacting the free acid with thionyl chloride. Pharmaceutical compositions of the compound I alone or with the usual excipients may be administered orally, parenterally or rectally when they show analgesic, antipyretic and anti-inflammatory activity.
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