| 摘要 |
The present invention relates to novel indene derivatives with the general formula I: <IMAGE> I wherein R1 is (a) a phenyl group optionally substituted with one or two groups selected from halogen, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulfonyl, dilower alkylamino, acylamino such as acetylamino, cyano, trifluoromethyl, trifluoromethoxy, pyrrole and dilower alkylpyrrole, (b) a polycyclic aromatic or heteroaromatic group, such as naphthalene or quinoline, (c) a heteroaromatic group such as thiophene, pyridine, and pyrrole, optionally substituted with one or more groups selected from halogen, lower alkyl, lower alkoxy, lower alkylthio, trifluoromethyl or trifluoromethoxy, R2 is selected from H, halogen, lower alkyl, benzyl, lower alkylthio, methoxy, lower alkylsulfonyl, dilower alkylsulfamoyl, acylamino such as acetylamino, benzylamino, dilower alkylamino, cyano, pyrrole, dilower alkylpyrrole, trifluoromethyl and trifluoromethoxy, R3 is CN, COOR4, -CON(R4)2 or COR4, where R4 is a lower alkyl group, and "n" is an integer of from 1-3 inclusive. The indene derivatives of formula I are, when R1 is as defined under (a) above, valuable intermediates which are useful in the preparation of pharmacologically effective indane and indene derivatives known from e.g. U.S. Pat. Nos. 4,443,448 and 4,525,360. Moreover, the invention relates to a method for the preparation of the compounds of formula I and to a method for the preparation of compounds of the following formula IV: <IMAGE> IV wherein R1, R2 and "n" are as defined above.
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