沈阳药科大学学报

2010, v.27;No.172(05) 361-364

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伊马替尼合成工艺的改进
Improved synthetic procedure of imatinib

昌盛;陈娜;董金华;
CHANG Sheng,CHEN Na,DONG Jin-hua(Key Laboratory of Structure-Based Drug Design & Discovery,Ministry of Education,Shenyang Pharmaceutical University,Shenyang 110016,China)

摘要(Abstract):

目的优化伊马替尼的合成工艺。方法以邻甲基苯胺、3-乙酰基吡啶、N,N-二甲基甲酰胺二甲基缩醛为起始原料,经硝化、缩合、环合、还原、酰胺化、取代等7步反应合成目标化合物。结果目标化合物结构经1H-NMR和MS谱确证结构,总收率为21.53%。结论新的工艺优化了反应条件,收率提高至70.2%。
Objective To optimize the synthetic procedure of imatinib.Methods Imatinib was prepared from o-toluidine,3-acetyl pyridine,N,N-dimethylformamide dimethyl acetal via nitration,condensation,cyclization,reduction,amidation and substitution reactions.Results The structure of target compound was confirmed by 1H-NMR and MS.The overall yield was 21.53%.Conclusions The synthetic process is optimized and the yield is added up to 70.2%.

关键词(KeyWords): 工艺改进;化学合成;伊马替尼
process improvement;chemical synthesis;imatinib

Abstract:

Keywords:

基金项目(Foundation):

作者(Authors): 昌盛;陈娜;董金华;
CHANG Sheng,CHEN Na,DONG Jin-hua(Key Laboratory of Structure-Based Drug Design & Discovery,Ministry of Education,Shenyang Pharmaceutical University,Shenyang 110016,China)

DOI: 10.14066/j.cnki.cn21-1349/r.2010.05.003

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