PLK1抑制剂(R)-BI-2536的合成  

Synthesis of PLK1 Inhibitor(R)-BI-2536

作　　者：陶燕[1] Tao Yan(Shaanxi Energy Institute,Shaanxi,712000)

机构地区：[1]陕西能源职业技术学院,陕西712000

出　　处：《当代化工研究》2024年第16期173-175,共3页Modern Chemical Research

摘　　要：为进一步优化PLK1抑制剂(R)-BI-2536的合成,以3-羟基-4-硝基苯甲酸为起始原料,经过甲基化、水解、缩合和还原反应4步合成中间体酰胺化合物,以2-氨基丁酸为起始原料,经过酯化、还原胺化、取代、关环和N-甲基化反应5步合成了中间体二氢喋啶酮类化合物,最后通过亲核取代反应完成了PLK1的抑制剂(R)-BI-2536的合成,总收率为19.2%,其结构由1H NMR和MS表征。The intermediate 3-methoxy-N-(1-methyl-4-piperidyl)-4-amino benzamide was synthesized by a four-step reaction including methylation,hydrolysis,condensation and reduction using 3-hydroxy-4-nitrobenzene acid as the starting material.The intermediate(7R)-2-chloro-7-ethyl-8-cyclopentyl-5-methyl-7,8-dihydropteridin-6(5H)-one was synthesized by a five-step reaction including esterification,amination,substitution,ringclosure and N-methylation reaction using L-2-aminobutyric acid as starting material.Finally,the PLK1 inhibitor BI2536 was obtained by nucle-ophilic substitution in total yield of 19.2%.The structure was confirmed by 1H NMR and MS.

关 键 词：(R)-BI-2536 PLK1抑制剂 合成 

分 类 号：O629.11[理学—有机化学]