吡唑并[1,5-a]吲哚类化合物的合成及其初步抗肿瘤活性的研究

Study on the synthesis and antitumor activity of pyrazolo[1,5-a] indole derivatives

以取代的邻溴苯乙酸为原料,经过一系列转化得到吡唑类化合物,再经Cu(I)催化下的分子内氨基化反应得到吡唑并[1,5-a]吲哚结构的中间体,最终得到吡唑并[1,5-a]吲哚类目标衍生物5 a、5b、5 c、5d,并采用MTT法评价目标物5的抗肿瘤活性.

Substituted 2-bromophenylacetic acids undergo a two-step reaction to afford pyrazoles,then,the following copper（I）-catalyzed intramolecular amination reaction affords pyrazolo[1,5-a] indole intermediates.Target products 5a,5b,5c,5d were obtained finally,and their bioactivities were evaluated by MTT methods.