抗肝癌药盐酸诺拉曲噻的合成*

目的：改进盐酸诺拉曲噻的合成工艺。方法：以2-溴4-硝基甲苯为原料经Sandmeyer法合成靛红、氧化开环、环合成喹唑啉酮和Ullmann反应合成了盐酸诺拉曲噻。结果：有关中间体及目标化合物的结构经必要的图谱确证，或经含量分析；总收率为28．8％。结论：本合成路线简洁，工业成本低，所得产品纯度高，适合于工业化生产。

Synthesis of nolatrexed dihydrochloride

Objective:To improve synthetic process of nolatrexed dihydrochloride.Methods: The target compound was synthesized from 2-bromo-4-nitrobenzene via several steps including Sandmeyer reaction,oxidative decyclization,cyclization,Ullmann reaction and acidification.Results:The struc- tures of related intermediates and the target compound were verified by spectroscopic techniques.The to- tal yield of target compound was for 28.8%.Conclusion:This economic and simplified synthetic process is feasible for further pilot manufacture.