抗肿瘤药替莫唑胺的合成

Synthesis of the Antitumour Drug Temozolide

以5-氨基-3H-咪唑-4-甲酰胺盐酸盐为原料,经重氮化反应合成5-重氮基-3H-咪唑-4-甲酰胺,然后在极性溶液和催化剂存在下与甲基异氰酸酯反应合成替莫唑胺,后者反应时间短,为20h,收率达76.5%。

Temozolide was synthesized from 5-amino-imidazole-4-carboxamide hydrochloride salt by diazotisation and in polar solvent cyclisation with methyl isocyanate in presence of catalyst . The yield of temozolide is 76.5% with reaction time 20 h.