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Citation: Jing Yunrong, Wei Jicheng. Study on the Synthesis of DNA-PK Inhibitor STL127705[J]. Chemistry, ;2019, 82(9): 860-863. shu

Study on the Synthesis of DNA-PK Inhibitor STL127705

Mudanjiang Normal University, Mudanjiang 157011

Received Date: 18 April 2019
Accepted Date: 17 May 2019

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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. By retrosynthetic analysis, using 4-chloro-2-methylsulfanyl-pyrimidine-5-carboxylic acid ethyl ester as the starting material, the target compound was prepared by a six-step reaction including ammonification, hydrolysis, amide condensation, cyclization, oxidation and substitution, with an overall yield of 36.8%, the purity of target product reached 95.5% and the product structure was confirmed by ¹H NMR, ¹³C NMR and MS.
- DNA-PK inhibitor,
- DNA repair,
- antitumor,
- synthetic process
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