| 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） |
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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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