新型吲唑类血管内皮生长因子受体抑制剂的合成

摘要

Objective To design and synthesize novel indazolylpyrimidine derivatives as antitumor drug candidates. Methods Five derivatives of indazolylpyrimidine benzenesulfonamide were synthesized from 2-ethylaniline via nitration, sulfonation, cyclization, nitroreduction , methylation and substitution in eleven steps. Their structures were identified by 1H-NMR and MS. Results and Conclusion Five novel target compounds and five novel intermediates were synthesized . This method can be generally used for synthesis of a series of novel indazolylpyrimidine derivatives as vascular endothelial growth factor receptor inhibitors.%目的 设计、合成一系列新型吲唑嘧啶类化合物,作为潜在的血管内皮生长因子抑制剂.方法 以邻乙基苯胺为原料,经硝化、磺化、环合、硝基还原、甲基化、取代等11步反应合成了5个吲唑嘧啶苯磺酰胺类衍生物,目标化合物和中间体经1H-NMR、MS进行结构鉴定.结果 与结论 设计合成的5个目标化合物及其中的5个中间体均未见文献报道.该合成方法简单可行,可作为一系列吲唑嘧啶类血管内皮生长因子抑制剂候选化合物的合成通法.