An Improved Synthesis of 4-(1-Piperazinyl)benzo[b]thiophene Dihydrochloride

doi:10.1021/acs.oprd.5b00027

	An Improved Synthesis of 4-(1-Piperazinyl)benzo[b]thiophene Dihydrochloride
	Wu, Chunhui 2; Chen, Weiming 1; Jiang, Dehui 1; Jiang, Xiangrui2 ; Shen, Jingshan2
刊名	ORGANIC PROCESS RESEARCH & DEVELOPMENT
	2015-04
卷号	19 期号:4 页码:555-558
ISSN号	1083-6160
DOI	10.1021/acs.oprd.5b00027
文献子类	Article
英文摘要	2-Chloro-6-fluorobenzaldehyde was converted to 4-(1-piperazinyl)benzo[b]thiophene dihydrochloride (18), an intermediate in the synthesis of brexpiprazole, via a five-step sequence in 54% overall yield. This procedure requires no expensive catalyst and avoids the side products produced in the coupling step in the reported process. Several kilograms of compound 18 were prepared using this economical and scalable process.
资助项目	Science and Technology Commission of Shanghai Municipality[14431905500] ; National Natural Science Foundation of China[81273366]
WOS关键词	CARBOXYLIC-ACIDS
WOS研究方向	Chemistry
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000353314900011
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/276581]
专题	药物化学研究室
通讯作者	Jiang, Xiangrui
作者单位	1.Topharman Shanghai Co Ltd, Shanghai 201209, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China;
推荐引用方式 GB/T 7714	Wu, Chunhui,Chen, Weiming,Jiang, Dehui,et al. An Improved Synthesis of 4-(1-Piperazinyl)benzo[b]thiophene Dihydrochloride[J]. ORGANIC PROCESS RESEARCH & DEVELOPMENT,2015,19(4):555-558.
APA	Wu, Chunhui,Chen, Weiming,Jiang, Dehui,Jiang, Xiangrui,&Shen, Jingshan.(2015).An Improved Synthesis of 4-(1-Piperazinyl)benzo[b]thiophene Dihydrochloride.ORGANIC PROCESS RESEARCH & DEVELOPMENT,19(4),555-558.
MLA	Wu, Chunhui,et al."An Improved Synthesis of 4-(1-Piperazinyl)benzo[b]thiophene Dihydrochloride".ORGANIC PROCESS RESEARCH & DEVELOPMENT 19.4(2015):555-558.