替拉扎明的合成方法改进

An Improved Synthesis of Tirapazamine

以邻硝基苯胺为起始原料,在50%氨基氰水溶液和浓盐酸共热,并且在氢氧化钠溶液中完成闭环反应生成3-氨基-1,2,4-苯并三嗪-1-氧化物中间体,最后氧化得到目标化合物的路线,总收率73%,纯度98.5%。

O - nitroaniline as the starting material, in 50% cyanamide aqueous solution, was healed with concentrated hydrochloric acid. In sodium hydroxide solution, the closed -loop reaction of 3 -amino -1,2,4- benzo -triazine -l -oxide intermediates was completed, and the final line of oxidation of target compounds was got, with the total yield of 73%, and the purity of 98. 5%.