| 摘要 |
1319026 Imidazoles MERCK & CO Inc 19 April 1971 [16 March 1970] 23404/71 Heading C2C Compounds of the formula or their acid addition salts (where R 1 is H or 1-5C-alkyl; R 2 is naphthyl, quinolyl or cinnolyl, a 5-6 membered hetero aryl ring optionally containing 1,2 or 3 O, N or S atoms and optionally substituted by 1-5C alkyl, 1-5C alkoxy or 1-5C-alkoxy-(1-5C-alkyl) or phenyl substituted by halogen, 1-5C alkyl, sulphamoyl, 1-5C - alkylsulphamoyl, 1-5C - alkoxy, 2-5C-alkanoylamino, NO 2 , NH 2 , 1-5C-alkyl- or di-(1-5C-alkyl)amino methylene dioxy, or a fused 3-6C alkylene bridge and R 5 is COOH, (1-6C - alkoxy)carbonyl, carbamoyl, 1-3C- alkyl- or di-(1-3C-alkyl)carbamoyl, CN, PhCO or 2-6C-alkanoyl; provided that when R 5 is COOH R 2 is not p- or m-nitrophenyl) are prepared by reacting an appropriate compound (I) wherein R 5 is CF 3 with alkali to give (I R 5 = COOH) then converting this group into other values of R 5 . 2 - (2,3 or 4 - Pyridyl) - 4(5) - trifluoromethylimidazole is prepared from 1,1-dibromo- 3,3,3-trifluoroacetone, 4-pyridine carboxaldehyde and ammonia. 2-(p-Fluorophenyl)-1-methyl- 4(and 5) - trifluoromethylimidazole is prepared by methylating 2-(p-fluorophenyl)-4(5)-trifluoromethylimidazole. The 1-ethyl derivative is similarly prepared. Pharmaceutical compositions contain compounds (I) in a form suitable for oral administration. Compounds (I) are antigout agents. |
