1-异丙基-3-异丙烯基-1H-吡唑并[3,4-d]嘧啶-4-胺的合成、表征及抗肿瘤活性

Zhu Zhoujing,Wang Yanjiao,Tong Hongjuan,Xu Xiaona,Liu Bin

Chemistry（2023）

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Abstract

以3-碘-1H-吡唑并[3,4-d]嘧啶-4-胺(2)为原料,经过N-烷基化反应得到中间体3-碘-1-异丙基-1H-吡唑并[3,4-d]嘧啶-4-胺(3),然后再与异丙烯基硼酸(4)发生Suzuki偶联反应,得到目标化合物1-异丙基-3-(异丙烯基)-1H-吡唑并[3,4-d]嘧啶-4-胺(1),两步反应总收率57.0％.产物及中间体结构经1H NMR、13C NMR及ESI-MS进行表征,同时,终产物结构进一步经X-射线单晶衍射确证.体外抗肿瘤活性测试表明,产物1对MCF-7、A549、PC-3、HepG2和SGC-7901增殖均有明显的抑制活性,特别是对于MCF-7细胞株的抑制活性IC50值达到10.6μmol/L.

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