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An improved synthesis of telmisartan via the copper-catalyzed cyclization of o-haloarylamidines

文献类型：期刊论文

作者Zhang, Junchi1,2; Li, Rui1,2; Zhu, Fuqiang3; Sun, Changliang3; Shen, Jingshan1,2
刊名RSC ADVANCES
出版日期2020-04-03
卷号10期号:23页码:13717-13721
DOI10.1039/d0ra00886a
通讯作者Sun, Changliang(changliang.sun@topharman.cn) ; Shen, Jingshan(shenjingshan@simm.ac.cn)
英文摘要A concise synthetic route was designed for making telmisartan. The key bis-benzimidazole structure was constructed via the copper-catalyzed cyclization of o-haloarylamidines. By adopting this approach, telmisartan was obtained in a 7-step overall yield of 54% starting from commercially available 3-methyl-4-nitrobenzoic acid, and the use of HNO3/H2SO4 for nitration and polyphosphoric acid (PPA) for cyclization in the reported literatures were avoided.
WOS关键词C-N ; BENZIMIDAZOLES ; NITRATION ; 2-IODOANILINES ; AROMATICS ; AMIDINES ; LIGANDS
资助项目Special Foundation of Chinese Academy of Sciences for Strategic Pilot Technology[XDA12050411] ; Science and Technology Commission of Shanghai Municipality[18431907100]
WOS研究方向Chemistry
语种英语
WOS记录号WOS:000530352000043
出版者ROYAL SOC CHEMISTRY
源URL[http://119.78.100.183/handle/2S10ELR8/280321]  
专题中国科学院上海药物研究所
通讯作者Sun, Changliang; Shen, Jingshan
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China
2.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
3.Topharman Shanghai Co Ltd, Bldg 1,388 Jialilue Rd,Zhangjiang Hitech Pk, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Zhang, Junchi,Li, Rui,Zhu, Fuqiang,et al. An improved synthesis of telmisartan via the copper-catalyzed cyclization of o-haloarylamidines[J]. RSC ADVANCES,2020,10(23):13717-13721.
APA Zhang, Junchi,Li, Rui,Zhu, Fuqiang,Sun, Changliang,&Shen, Jingshan.(2020).An improved synthesis of telmisartan via the copper-catalyzed cyclization of o-haloarylamidines.RSC ADVANCES,10(23),13717-13721.
MLA Zhang, Junchi,et al."An improved synthesis of telmisartan via the copper-catalyzed cyclization of o-haloarylamidines".RSC ADVANCES 10.23(2020):13717-13721.

入库方式： OAI收割

来源：上海药物研究所

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