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METHOD FOR PRODUCING NUCLEOSIDE 8-OXO-2`-DEOXYGUANOSINE (8-oxo-dG)

机译:制备核苷8-OXO-2`-脱氧鸟苷(8-氧代-dG)的方法

摘要

FIELD: chemistry.SUBSTANCE: invention relates to a synthesis method of 8-oxo-2'-deoxyguanosine (8-oxo-dG), which can be used in pharmaceutical and chemical industry. Method is carried out by acylation of 8-bromo-2'-nucleoside-deoxyguanosine (8-Br-dG) mixture of acetic anhydride and sodium acetate in a polar aprotic organic solvent in the presence of a N-methylimidazole catalyst followed by hydrolysis of an acyl group, wherein the solvent used is N-dimethylformamide, to which pyridine is added to a final concentration of 1.8 mM to prevent apurination, reaction is carried out at 120–155 °C for 12–28 hours, obtaining desired product (8-oxo-dG) is carried out by removing acyl groups using alkaline hydrolysis in 0.1–1.5 M aqueous NaOH solution.EFFECT: novel efficient method of producing a valuable product.1 cl, 2 dwg, 6 ex
机译:技术领域本发明涉及8-氧代-2'-脱氧鸟苷(8-氧代-dG)的合成方法,其可用于制药和化学工业。该方法是在N-甲基咪唑催化剂存在下,在极性非质子有机溶剂中将乙酸酐和乙酸钠的8-溴-2'-核苷-脱氧鸟苷(8-Br-dG)混合物酰化,然后进行水解。酰基,其中使用的溶剂为N-二甲基甲酰胺,向其中添加吡啶至终浓度为1.8 mM以防止嘌呤化,在120-155°C下反应12-28小时,得到所需的产物(8 -oxo-dG)是通过在0.1–1.5 M NaOH水溶液中进行碱水解来除去酰基基团而实现的。效果:生产有价值产品的新型有效方法。1cl,2 dwg,6 ex

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