含哌嗪基7-溴噻吩并[3,2-d]嘧啶抗癌试剂的设计与合成

Design and synthesis of 7-bromothieno[3,2-d]pyrimidine derivatives containing piperazine unit as anticancer agents

为寻找以蛋白酪氨酸激酶为靶点的新型抗癌试剂,本文设计与合成了系列含哌嗪基的7-溴噻吩并[3,2-d]嘧啶衍生物。以巯基乙酸为原料,经六步反应得4-氯-7-溴噻吩并[3,2-d]嘧啶母核,再与不同的哌嗪衍生物在添加三乙胺作碱的条件下反应,制备了五个未见报道的含哌嗪基7-溴噻吩并[3,2-d]嘧啶化合物。结构经1H NMR和HRMS表征。

In the quest for novel protein tyrosine kinase inhibitors as putative anti-cancer agents,a series of 7-bromothieno[ 3,2-d] pyrimidines containing a piperazine unit were designed and sgnthesized. Starting from mercaptoacetic acid,7-bromo-4-chlorothieno [ 3,2-d ] pyrimidine was obtained by 6-step reactions. Five novel 7-bromothieno [ 3,2-d] pyrimidines containing a piperazine unit were synthesized through the reactions between the 7-bromo-4-chlorothieno [ 3,2-d ] pyrimidine and piperazine derivatives in the presence of Et3N. These new compounds were characterized with 1H NMR and HRMS.