替莫唑胺的合成及抗肿瘤活性

Synthesis of Temozolomide and Its Antitumor Activity

以 5 -氨基 - 3H-咪唑 - 4-甲酰胺盐酸盐为原料 ,经重氮化、与异氰酸甲酯进行环合反应生成替莫唑胺 ,并对其进行抗肿瘤活性试验。结果显示本品具有明显的体外抑瘤活性 ,可显著抑制小鼠 S1 80 实体瘤重、延长艾氏腹水瘤小鼠的生存时间。

Temozolomide was synthesized from 5-amino-3H-imidazole-4-carboxylamide by diazotization and cyclization with methyl isocyanate in an overall yield of 72%. The antitumor activity test showed that it inhibited tumor in vitro and could inhibit S 180 tumor in mice and enlongate the living time of ehrlich ascites mice.