| 摘要 |
A description is given here of novel solid and stable derivatives of (-)-verbenone having formula (I) wherein, when X=O Z=H, =CHAr, =C(OH)COOEt, =NOR; Y=H, NH2, NH3+X1-, NHCOAr, NHCOR, NHCONHR, NHCONHAr, X1-=pharmaceutically acceptable anion; Ar-aryl or heteroaryl, preferably phenyl, 4-chlorophenyl, 2-furyl, 2-thienyl, 2-hydroxyphenyl, 2-acetoxyphenyl; R=H, C1-C4 alkyl, C4-C6 cycloalkyl, CH2COOH, CH2COOEt, CH2COCH3, CH2CN, CH2COCH2COOEt, CH2C6H5; and, when X=dimethylamino, diethylamino, pyrrolidino, piperidino or morpholino: Y=H; Z=H, CONHAr, COHNR; Ar=aryl, preferably phenyl; R=H, C1-C4 alkyl, C4-C6 cycloakyl. A description is also given of the processes for the preparation of these derivatives and of the novel intermediates used in those processes. The novel derivatives are characterized by their solubility in water; some of them also have a high anti-inflammatory activity.
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