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

doi:10.1039/d0ra00886a

	An improved synthesis of telmisartan via the copper-catalyzed cyclization of o-haloarylamidines
	Zhang, Junchi 1,2; Li, Rui 1,2; Zhu, Fuqiang 3; Sun, Changliang 3; Shen, Jingshan 1,2
刊名	RSC ADVANCES
	2020-04-03
卷号	10 期号:23 页码:13717-13721
DOI	10.1039/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.
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关键词	C-N ; BENZIMIDAZOLES ; NITRATION ; 2-IODOANILINES ; AROMATICS ; AMIDINES ; LIGANDS
WOS研究方向	Chemistry
语种	英语
出版者	ROYAL SOC CHEMISTRY
WOS记录号	WOS:000530352000043
内容类型	期刊论文
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.