中文摘要：

目的对PI3K-δ抑制剂idelalisib的合成工艺进行研究。方法以2-氟-6-硝基苯甲酸为起始原料，经氯化、与苯胺缩合、水合肼还原、与（2s）-2-{[（1，1-二甲基乙氧基）羰基]氨基}丁酸缩合得到N-{（1S）-1-[（{3-氟-2-[（苯基氨基）羰基]苯基}氨基）羰基]丙基}氨基甲酸-1，1-二甲基乙基酯，再经环合、脱保护基得到2-[（1S）-1-氨基丙基]-5-氟-3-苯基4（3H）-喹唑啉酮，最后与6-溴-9H-嘌呤发生亲核取代反应得到目标化合物idelalisib。结果与结论idelalisib的总收率为30．8％（以2-氟-6-硝基苯甲酸计），纯度为99．9％，其结构经IR、MS、^1H．NMR、^13C—NMR确证。该路线未见文献报道，反应原料易得，反应条件温和，操作简便，为其中试放大奠定了基础。

英文摘要：

A new synthetic route to idelalisib has been developed after summarizing all the synthetic methods reported in literatures. Starting from 2-fluoro-6-nitrobenzoic acid, idelalisib was obtained by condensation, reduction,condensation,cyclization, deprotection and substitution with the total yield of 30. 8% （calculated by 2-fluoro-6-nitrobenzoic acid）. The structure of idelalisib was confirmed by IR, MS, ^1H-NMR, ^13C-NMR, and the structures of some interme-diates were confirmed by MS and ^1H-NMR. The improved route has perfect innovation and practicality, and it also has some advantages such as cheap, mild reaction conditions, high yield and simple operation, which is suitable for the large-scale production.