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从水杨腈出发,经醚化、两次成环、氯化制得4-氯-苯并[4,5]呋喃[3,2-d]嘧啶(5);5与5-取代-2-巯基-1,3,4-噻二唑反应,合成了7个新的含噻二唑的苯并[4,5]呋喃[3,2-d]嘧啶衍生物.其结构经1HNMR,13CNMR,IR和MS表征,培养并测定化合物6a的晶体结构.采用MTT法进行化合物抑制PC3癌细胞体外活性测试,结果表明所合成的化合物具有不同程度的抑制PC3癌细胞活性,其中化合物6b在10μmol?L-1浓度下对PC3的抑制率为89.2%.
Starting from the salicyonitrile, etherification, cyclization and chlorination twice to give 4-chloro-benzo [4,5] furo [3,2-d] Thiazole, seven novel benzo [4,5] furan [3,2-d] pyrimidine derivatives containing thiadiazole were synthesized and their structures were confirmed by 1HNMR, 13CNMR , IR and MS were used to culture and determine the crystal structure of compound 6a.MTT method was used to inhibit the activity of PC3 cancer cells in vitro.The results showed that the compounds have different degrees of inhibition of PC3 cancer cell activity, The inhibition rate of PC3 at the concentration of L-1 was 89.2%.