| 摘要 |
1331505 Thiophen-acetic acid derivatives ROUSSEL UCLAF 11 Nov 1970 [12 Nov 1969] 53561/70 Heading C2C Novel compounds I in which R is H or 1-4C alkyl; R<SP>1</SP> is H or straight or branched-chain 1-4C alkyl; R<SP>2</SP> is H, substituted or unsubstituted alkyl; alkali or alkaline earth metal, Al or dialkylammonium and Ar is a substituted or unsubstituted phenyl radical, cyclohexyl or heterocyclyl are prepared by reaction of compounds II with an appropriate acylating agent derived from ArCOOH in the presence of a Lewis acid followed by esterification or salt formation. Intermediates isolated are α-methyl-α-hydroxy- 3-methyl-thiophen-2-acetic acid, prepared from the appropriate thiophen-2-glyoxylic acid and methyl magnesium iodide; α-methyl-3-methylthiophen-2-acetic acid, prepared by reduction of the former intermediate; 4-methyl-thiophen-2- carboxylic acid chloride, prepared by reaction of the acid with SOCl 2 ; α-diazo-4-methylacetothinone, prepared from the acid chloride and diazomethane; ethyl 4-methyl-thiophen-2- acetate, prepared by reaction of the diazo compound with silver benzoate in triethylamine and 4-methyl-thiophen-2-acetic acid, prepared by hydrolysis of the ethyl ester. Pharmaceutical compositions having antiinflammatory and a analgesic properties comprise a compound I together with an appropriate diluent and/or carrier for enteral, parenteral or topical administration. |
