景云荣,魏继承.化学通报,2019,82(9):860-863.
DNA依赖的蛋白激酶抑制剂STL127705的合成工艺研究
Study on the Synthesis of DNA-PK Inhibitor STL127705
投稿时间:2019-04-18  修订日期:2019-05-17
DOI:
中文关键词:  DNA-PK抑制剂 DNA修复 抗肿瘤 合成方法
英文关键词:DNA-PK  inhibitor, DNA  repair, antitumor, synthetic  process
基金项目:黑龙江省人社厅留学回国人员择优资助项目,牡丹江师范学院科研项目(MNUB201405)
作者单位E-mail
景云荣 牡丹江师范学院 swxjyr@126.com 
魏继承 牡丹江师范学院  
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中文摘要:
      DNA依赖的蛋白激酶(DNA-PK)是肿瘤治疗的一个潜在靶点,其抑制剂具有增强放化疗敏感性的作用。STL127705是一种有效的DNA-PK抑制剂,本文采用逆合成分析,以2-甲硫醚-4-氯嘧啶-5-基甲酸乙酯为起始原料,先后经过氨化、水解、酰胺缩合、合环、氧化、取代等6步反应制备得到目标化合物,总收率为36.8%,纯度达到95.5%,产物结构通过1H-NMR、13C-NMR、MS等表征。
英文摘要:
      DNA-dependent protein kinase (DNA-PK) is a potential target for tumor therapy. DNA-PK inhibitor can enhance the sensitivities of tumor cells against chemotherapy and radiotherapy. STL127705 is an effective inhibitor of DNA-PK. It was prepared by retrosynthetic analysis, using 4-chloro-2-methylsulfanyl-pyrimidine-5-carboxylic acid ethyl ester as the starting material, followed by 6 steps reaction including ammonification, hydrolysis, amide condensation, cyclization, oxidation and substitution, with an overall yield of 36.8%, the purity reached 95.5% and the structure of the target compound was confirmed by 1H-NMR, 13C-NMR and MS.
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