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氢溴酸吡西替尼合成新方法

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目的 介绍一种合成氢溴酸吡西替尼的新方法。方法 以4-氯-1H-吡咯并[2,3-b]吡啶-5-甲腈为原料,经缩合反应,取代反应,水解反应,最后成盐得氢溴酸吡西替尼。结果 本方法总收率61。8%,纯度99。2%。结论 本方法安全环保,收率高,适合工业化生产。
New method for the preparation of peficitinib hydrobromide
Objective To introduce a new method for synthesize peficitinib hydrobromide.Methods Peficitinib hydrobromide was synthesized from 4-chloro-1H-pyrrolo[2,3-b]pyridine-5-carbonitrile via the reactions including con-densation reaction,substitution reaction,hydrolysis reaction and salt formation.Results The method had been successfully implemented to prepare the target compound in 61.8%overall yield and 99.2%area purity.Conclusion The method was suitable for industrial production with safety and environmental protection high yield.

Peficitinib hydrobromideSynthesisAlkylation

庄红伟、张庆、于帅、邓成龙、李国锋、张红卫

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齐鲁制药有限公司,山东济南 250100

氢溴酸吡西替尼 合成 烷基化

2024

药学研究
山东省药品检验所 山东省药学会

药学研究

CSTPCD
影响因子:0.653
ISSN:2095-5375
年,卷(期):2024.43(9)