| 摘要 |
5-methyl-isoxazole-4-carboxanilides (I; R1 = H, OCH3, F; R2 = H, Cl, CF3, CH3, F; R3 = Cl, Br, F, CF3 NO2, OCF2CHF2, OCH3, OC2H5, OCF2-CHClF, SCH3, CH3, CN), useful as antiinflammatory agent and analgesics, were prepd. by cyclocondensation of II and III. Thus, reaction of MeCOCH2CONHC6-H3Cl2-3, 4 with HC(OEt)3 in refluxing Ac2O gives after 1.5 hr 83% MeCOC(:CHOEt)CONHC6H3Cl2-3,4(IV). Reaction of IV with H2NOHHCl in MeOH-aq. NaOH at room temp. gives after 4 hr 97.5% I(R1 = 3-Cl; R2 = 4-Cl).
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