| 摘要 |
Procedure for the preparation of imidazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, where -X- is -CO- or -CH2-; and -Y- is CH-Imz or C=CH-CH2-Imz, Imz being the radical 1-imidazolyl; -R is -H, C1-C4 alkyl, -(CH2CH2O)n-H with n=1,2,3, -(CHOH)m-H with m=2,3,4, which comprises a nucleophilic substitution reaction in which an outgoing group is replaced by imidazole, in a dipolar aprotic solvent, such as acetonitrile or dimethylformamide, in the presence of a base and, if it is desired to obtain a salt of (I), the subsequent addition of the corresponding acid. The products of formula (I) can also be obtained by interconversion inter se; esters by esterification of carboxylic acids, the latter by hydrolysis of the former, and primary alcohols by reduction of esters with aluminium and lithium hydride. The products of formula (I) are analgesic/anti-inflammatory agents which do not have any ulcerogenic side effects at the maximum doses tried, and which - in some cases - even have anti-ulcer activity. <IMAGE>
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