论文部分内容阅读
通过2-氨基-3-氰基噻吩与三氟乙酸、三氯氧磷反应“一锅法”制得2-三氟甲基-4-氯噻吩并[2,3-d]嘧啶,收率为60%,再与2-氨基-5-(取代苄硫基)-1,3,4-噻二唑发生芳香族亲核取代反应合成10个含噻二唑环噻吩并[2,3-d]嘧啶类含氟衍生物,收率为64%~75%。目标化合物的结构经红外光谱、核磁共振氢谱、质谱与元素分析表征,并采用MTT法对其进行初步的体外抗肿瘤活性筛选。结果表明,化合物Ⅳc和Ⅳf对Hep G2和BGC-823细胞的抑制活性高于对照样吉非替尼。
2-Trifluoromethyl-4-chlorothieno [2,3-d] pyrimidine was prepared by reaction of 2-amino-3-cyanothiophene with trifluoroacetic acid and phosphorus oxychloride. The yield was 60%. Aromatic nucleophilic substitution reaction with 2-amino-5- (substituted benzylthio) -1,3,4-thiadiazole was also performed to synthesize 10 thiadiazole- 3-d] pyrimidine derivatives with a yield of 64% -75%. The structures of target compounds were characterized by IR, 1HNMR, MS and elemental analysis, and their anti-tumor activities were screened by MTT assay in vitro. The results showed that the inhibitory activity of compounds Ⅳc and Ⅳf on Hep G2 and BGC-823 cells was higher than that of gefitinib.