Andreani A, Bonazzi D, Rambaldi M, Guarnieri A, Andreani F, Strocchi P, Montanaro N
J Med Chem. 1977 Oct;20(10):1344-6. doi: 10.1021/jm00220a023.
The Vilsmeier and the Arndt-Eistert reactions have been employed for the synthesis of 1-phenyl-2-chloroindole-3-acetic acid (4). The antiinflammatory activity of 2-chloroindole-3-carboxylic acid (1), 1- methyl-2-chloroindole-3-carboxylic acid (2), 1-phenyl-2-chloroindole-3-carboxylic acid (3), and 4 was compared with the activity of indomethacin in the carrageenin rat edema. The best results are given by compounds 1 and 2 bearing H or CH3 at position 1 and COOH at position 3.
维尔施迈尔反应和阿恩特-艾司特反应已被用于合成1-苯基-2-氯吲哚-3-乙酸（4）。将2-氯吲哚-3-羧酸（1）、1-甲基-2-氯吲哚-3-羧酸（2）、1-苯基-2-氯吲哚-3-羧酸（3）和4的抗炎活性与吲哚美辛在角叉菜胶所致大鼠水肿中的活性进行了比较。在1位带有H或CH₃且在3位带有COOH的化合物1和2给出了最佳结果。
