| 摘要 |
<p>1374345 Oxazole derivatives GRUPPO LEPETIT SpA 14 Dec 1972 [7 Aug 1972] 53966/72 Heading C2C Novel oxazole derivatives of the formula wherein A is cyclohexyl, thienyl or phenyl optionally substituted by one or more halogen atoms, or C 1-6 alkyl, halo-C 1-6 alkyl, C 1-6 alkoxy, NO 2 , CN, NH 2 , carbamoyl, sulphamoyl or carboxy radicals, and one of the radicals R 1 and R 2 is C 1-6 alkyl and the other is CON(R 3 )R 4 , wherein R 3 is H, C 1-6 alkyl, C 2-6 alkenyl, cycloalkyl, aryl, aryl-C 1-6 alkyl, hydroxy-C 1-6 alkyl, acyloxy-C 1-6 alkyl, OH, NH 2 , C 1-6 alkylideneamino, cycloalkylideneamino, or aralkylideneamino, and R 2 is H, C 1-6 alkyl, C 2-6 alkenyl, cycloalkyl, aryl, aryl-C 1-6 alkyl, hydroxy- C 1-6 alkyl or acyloxy-C 1-6 alkyl, or R 3 and R 4 , together with the N atom to which they are attached form a 5 to 7 membered saturated heterocyclic ring optionally containing further N, O or S atoms, are prepared by reacting the appropriate C 1-6 alkyl 4-(or 5-)-oxazolecarboxylates or 4- (or 5-)-oxazolecarboxylic acid halides with amines of the formula Alternatively compound in which R 3 is C 1-6 alkylideneamino, cycloalkylideneamino or aralkylideneamino may be obtained by reacting compound in which R 3 is NH 2 with the corresponding aldehydes or ketones, and those in which R 3 and/or R 4 is acyloxy-C 1-6 alkyl by acylating the corresponding hydroxy compounds. Ethyl 2 - phenyl - 4 - methyl - 5 - oxasolecarboxylate, 5 - methyl - 2 - phenyl - 4 - oxazolecarboxylic acid chloride, ethyl 5 - methyl - 2 - (2- thienyl) - 4 - oxazolecarboxylate, ethyl 5 - methyl- 2 - (4 - fluorophenyl) 4 - oxazolecarboxylate, 2- (4 - hclorophenyl) - 5 - methyl - 4- oxazolecarboxylic acid chloride, 5 - methyl - 2 - (p - tolyl) - 4- oxazolecarboxylic acid chloride, and 2-cyclohexyl 5 - methyl - 4 - oxazolecarboxylic acid chloride are obtained by known methods. Pharmaceutical compositions, having antiinflammatory and analgesic activities, contain the above novel compounds together with pharmaceutically acceptable carriers.</p> |
