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Improved synthesis of raltegravir

文献类型：期刊论文

作者GUO Di-liang2; LIU Guan-nan1; LI Jian1; ZHOU Yu1; XU Jin-yi2; JIANG Hua-liang1; LIU Hong2
刊名Journal of China Pharmaceutical University
出版日期2009
卷号40期号:4页码:297-301
关键词raltegravir HIV-1 integrase raltegravir synthesis process research
ISSN号1000-5048
其他题名Raltegravir的合成工艺研究
文献子类Article
英文摘要Aim: To develop a practical synthetic route of raltegravir, a drug for HIV treatment. Methods: Raltegravir was synthesized through an eight-step process including aminonitrile formation, protection with benzyloxy-carbonyl group, conversion of the nitrile to the amidoxime, cyclization to form hydroxypyrimidinone, N-methyla-tion, amidation with microwave-assistance, deprotection, amidation with acyl chloride. Results: The overall yield of the eight-step synthesis is about 12. 0% and the structure of the target compound was confirmed by ~1H NMR, ~(13)C NMR, LR-MS and HR-MS. Conclusion: The reported synthetic process of raltegravir highlights the advantages in terms of readily available starting materials, convenient operation and low cost.
资助项目the National High Technology Research and Development Program of China(863 Program)[00000000]
WOS研究方向Pharmacology & Pharmacy (provided by Clarivate Analytics)
语种中文
CSCD记录号CSCD:3739690
源URL[http://119.78.100.183/handle/2S10ELR8/267996]  
专题中国科学院上海药物研究所
作者单位1.Drug Discovery and Design Center, Shanghai 201203, China.
2.Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.;
推荐引用方式
GB/T 7714		 GUO Di-liang,LIU Guan-nan,LI Jian,et al. Improved synthesis of raltegravir[J]. Journal of China Pharmaceutical University,2009,40(4):297-301.
APA GUO Di-liang.,LIU Guan-nan.,LI Jian.,ZHOU Yu.,XU Jin-yi.,...&LIU Hong.(2009).Improved synthesis of raltegravir.Journal of China Pharmaceutical University,40(4),297-301.
MLA GUO Di-liang,et al."Improved synthesis of raltegravir".Journal of China Pharmaceutical University 40.4(2009):297-301.

入库方式： OAI收割

来源：上海药物研究所

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