XL765.discovered by Exelixis and Sanofi-aventis,is an orally available inhibitor of phosphoinosi-tide-3-kinase(PI3K) that offer considerable therapeutic potential. According to the synthetic method of XL765 in patent, its synthetic route is established, and the synthetic process is investigated and optimized thoroughly. XL765 was prepared from 1,2-diaminobenzene and oxalic acid via six steps including cycliza-tion.chlorination, chloro-sulfonation, sulfonylation, two times nucleophilic substitution, reduction of nitro group and acylation to give the target compound. Its structure and some intermediates were confirmed by 1H-NMR and MS. The total yield was 31. 5% (calculated by 1,2-diaminobenzene),higher than 25.5% reported in the patent.%目的 改进磷脂酰肌醇-3-激酶(PI3K)抑制剂XL765的合成工艺..方法:以邻苯二胺、草酸为起始原料经过环合、氯代、氯磺化、磺酰化、取代、还原以及酰胺化制得XL765.结果与结论经过6步反应合成目标化合物XL765,化学结构经1H-NMR及MS确证.对其中多步反应条件进行了工艺考察及优化,总收率为31.5％(以邻苯二胺计),高于文献报道收率(25.5％).
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