抗肿瘤药PD168393的合成研究

A Study on the Synthesis of Anticancer agent PD168393

目的改进新型喹唑啉类抗肿瘤药PD168393的合成工艺方法。方法以5-硝基-2-氨基苯甲酸为起始原料经环化、活化、胺基化、还原等步骤得到6-氨基-4-(3-溴苯胺基)喹唑啉,与丙烯酰氯缩合得到PD168393。结果经过5步反应得到白色粉末固体。结论新的合成方法原料易得,操作方法简便,副产物生成少,易分离纯化,总产率14%。

Objective To improve the synthesis of the anti-tumor agent PD168393 of new quinazoline derivatives.Methods With 5-nitro-this-2-aminobenzoic acid as the raw material,the target compound was obtained through cyclization,activation,amination,reduction and condensation.Results The target compound was synthesized in five steps to produce a white powder solid.Conclusion The new synthesis method is simple and mild.Starting materials are readily available with a total yield of 14%.