摘要/Abstract
甲磺酸普喹替尼是一种新颖的磷脂酰基醇3-激酶（PI3K）抑制剂，临床实验结果显示对肿瘤治疗有较好的效果.报道了公斤级合成该抑制剂的方法，以2，6-二氯嘌呤为起始原料，通过氨基上保护、区域选择性SN2亲核取代反应、Buchwald-Hartwig偶联反应，氨基脱保护成盐合成了甲磺酸普喹替尼，该法操作简单，总收率达到48%，为其放大生产提供了有效途径.
关键词: PI3K抑制剂, 普喹替尼, 合成
Puquitinib mesylate is a novel phosphatidylinositol 3-kinases (PI3K) inhibitor, which has been shown to be effective in the treatment of cancer. A convenient protocol for the synthesis of the compound at kilogram scale is described, using 2,6-dichloropurine as starting material through amino-protection, SN2 reaction with high regioselectivity, Buchwald-Hartwig coupling reaction, amino-deprotection and salt-forming reaction. The process is easy to operate and provides an effective way at kilogram scale produce with 48% yield in total.
Key words: PI3K inhibitor, puquitinib, synthesis
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