Gaviraghi G, Banfi S, Cornelli U, Pinza M, Pifferi G
Farmaco Sci. 1977 Apr;32(4):286-95.
The synthesis of 3-chloro-4-cyclopropylmethoxyphenylacetic acid (I) from 3-chloro-4-hydroxyacetophenone (III) by the etherification with cyclopropylmethyl bromide and by the Willgerodt reaction is described. The alpha-methyl homologue (II) was also prepared from 4-benzyloxy-3-chlorophenylacetate (VIII). The antiinflammatory, analgesic and antipyretic activities of the lysine salts of (I) (ISF 2508) and (II) (ISF 2606) were tested in comparison with alclofenac and phenylbutazone. The new ocmpounds compare favourably with the standards; in particular ISF 2508 was selected for further pharmacological studies.
描述了由3-氯-4-羟基苯乙酮（III）通过与环丙基甲基溴进行醚化反应以及威尔格罗德特反应合成3-氯-4-环丙基甲氧基苯乙酸（I）的方法。α-甲基同系物（II）也由4-苄氧基-3-氯苯乙酸酯（VIII）制备。将（I）（ISF 2508）和（II）（ISF 2606）的赖氨酸盐的抗炎、镇痛和解热活性与阿氯芬酸和保泰松进行了比较测试。新化合物与标准品相比具有优势；特别是ISF 2508被选用于进一步的药理研究。
