5,6,7,8-四氢吡啶并3,4-d 嘧啶衍生物的合成

摘要

Based on benzylamine as raw material,a series of novel 5,6,7,8-tetrahydro-pyrido[3,4-d] pyrimidine derivatives were designed and synthesized through several step reactions including substitution,condensation,hydrolysis and deprotection. The struc-tures of these compounds were characterized by 1 H NMR,13 C NMR,MS and elemental analysis. Antitumor activities of these com-pounds were evaluated according to the vitro and antitumor activity studies. The results indicated that these compounds had a certain inhibitory activity in MCF-7 human breast cancer cells,in which the inhibitory activity of 10a and 10d reached average level.%以苄胺为原料,经过取代,缩合,水解,脱保护等步骤,设计合成了一系列新型的5,6,7,8-四氢吡啶并[3,4-d]嘧啶类化合物。通过1 H NMR,13 C NMR,MS和元素分析确证了其结构。并且对其体外抗肿瘤活性进行了研究,发现该类化合物对乳腺癌细胞MCF-7具有一定的抑制活性,其中化合物10a和10d的抑制活性达到了中效水平。