| 摘要 |
1347893 Trifluoromethyl-diaryl-imidazoles PFIZER Inc 19 April 1971 [16 Nov 1970] 25321/71 Heading C2C Novel compounds of the formulµ and their acid addition salts, wherein Ar and Ar<SP>1</SP> are each the same or different and are furyl, thienyl, pyridyl, phenyl or phenyl substituted by F, Cl, Br, alkyl, alkoxy, or alkylthio each containing 1 to 4 carbons, or 3,4- dimethoxy, R 1 is H, C 1-4 alkyl or C 3-4 alkenyl, may be obtained by heating an α-diketone Ar-COCO-Ar<SP>1</SP> with an aldehyde CF 3 CHO and ammonium acetate to yield I, or ArCOCOCF 3 with Ar<SP>1</SP>CHO and ammonium acetate to II and III. An alternative method comprises condensation of an α-haloketone ArCOCHXAr<SP>1</SP> (where X is Cl or Br) with an amidine to yield I or ArcOCHXCF 3 with to yield II and III. The intermediate diaryl α-diketones are obtained by selenium dioxide oxidation of the corresponding aryl arylmethyl monoketone; C 6 H 5 .CO.CO.CF 3 is obtained by selenium dioxide oxidation of C 6 H 5 CH 2 COCF 3 . The aryl arylmethyl monoketones are obtained by methods analogous to the synthesis of panisyl p-methylphenyl ketone by Friedel Crafts reaction of p-tolylacetyl chloride and anisole in the presence of AlCl 3 in CS 2 . 4-Picolyl 2- pyridyl ketone is obtained from 4-picoline and methyl 2-picolinate. Pharmaceutical compositions, useful as antiinflammatory agents, comprise a compound of Formulµ I, II or III and an acceptable carrier, in forms suitable for oral or parenteral administration. |
