| 摘要 |
<p>Aromatic sulphoxides of general formula (I):- Het = a hetero aromatic ring structure of 3 rings and 5-6 atoms; this ring may contain one or more N or S; or O together with one or more O, S or N Y = halogen, alkyl, alkenyl, cycloalkyl, amino, alkylamino, dialkylamino, alkoxy, hydroxy, mercapto, alkylmercapto or nitro; n = 0, 1 or 2; R2 and R3 = H, alkyl or alkenyl; R4 = alkyl or alkenyl. Preferred compounds have R2 and R3 = H; R4 = alkyl. Antipyretic-, analgesic- and anti-inflammatory activity with low toxicity. May be used against diseases symptomatically characterised by pain, fever and/or inflammation. (A) 2-Chloromethylthiazole 2-Hydroxymethylthiazole (X) A mixture of 14.2 mol. thiazole and 50 ml. 40% aqueous formalin is heated to ca. 120 deg.C. for 8 hrs. while stirring. After cooling and acidifying the mixture is extracted with ether. The aqueous solution is made alkaline with solid K2CO3 and the product extracted 4 times with ether. After drying and evap. the residue is taken up in a mixture of conc. HCl/H2O = 1:1, filtered and evaporated. Treatment of the residue with ethanol gives 1.76 g. of the desired product. (B) 2-Chloromethylthiazole 1.76 g. of (X) are suspended in 16 ml. chloroform and in 5 mins. a solution of 0.03 mol. thionyl chloride in 10 ml. chloroform is added and the mixture refluxed for 1 3/4 hours. After cooling and evap. the residue is made alkaline and extracted with ether. Working up gives the desired product.</p> |
