Ⅰ.Study On The Synthesis Of Uracil Derivatives Ⅱ.Study On The Synthesis Of 1, 4-Dihydro-s-Tetrazine Derivatives And Their Antitumor Activity

The dissertation includes two parts as follows:In the first part, the synthesis of the uracil derivatives : 5-methoxyuracil and 5-methyluracil(thymine) was investigated, and the reaction conditions were optimized, thus the overall yields were higher than before.In part two, the synthesis of tetrazine and its derivatives, the corresponding antitumor activities were also studied. Three aspects were included here:The derivatives of dihydrol,2,4,5-tetrazine-3,5-dicarboxylic acid were synthesized via three different routes:(1) four new compounds were synthesized via the reaction bet ween dihydrol,2,4,5-tetrazine-3,5-dicarboxylic acid, thionyl chloride and corresponding alcohol ;(2) first ,dimethyl dihydro-1,2,4,5-tetrazine-3,5-dicarboxylate wer e synthesized, then ,another four new compounds were obtained t hrough the alcoholysis under the catalyst ;(3) three acylamines were got through the ammonolysis betw een dimethyl dihydro-1,2,4,5-tetrazine-3,5-dicarboxylate and amines. Those 11 new compounds were determined throughMS, 1 HNMR, 1R and element analysis.The antitumor activities in vitro of most prepared compounds were screened . However, the activities of those compounds were not good, some of them showed certain activities in high concentration, while in low concentration they were unavail.