Copper-Mediated ortho-C-H Amination Using DMF as the Amine Source

doi:10.1021/acs.orglett.1c03223

	Copper-Mediated ortho-C-H Amination Using DMF as the Amine Source
	Cheng, Tai-Jin 1,2; Chen, Jun-Jie 1; Wu, Peng 3; Xu, Hui 1; Dai, Hui-Xiong 1,2
刊名	ORGANIC LETTERS
	2021-11-05
卷号	23 期号:21 页码:8505-8509
ISSN号	1523-7060
DOI	10.1021/acs.orglett.1c03223
通讯作者	Dai, Hui-Xiong(hxdai@simm.ac.cn)
英文摘要	We report herein a copper-mediated ortho-C-H amination of anilines using oxalamide as the directing group and DMF as the amination reagent. This protocol tolerates various functional groups and shows good heterocyclic compatibility. Late-stage dimethylamination of drugs demonstrated the synthetic practicality of the protocol. Mechanistic experiments indicate that a radical pathway may be involved in the reaction.
资助项目	Shanghai Institute of Materia Medica ; Chinese Academy of Sciences ; National Natural Science Foundation of China[21772211] ; National Natural Science Foundation of China[21920102003] ; Youth Innovation Promotion Association CAS[2014229] ; Youth Innovation Promotion Association CAS[2018293] ; Institutes for Drug Discovery and Development, Chinese Academy of Sciences[CASIMM0120163006] ; Science and Technology Commission of Shanghai Municipality[17JC1405000] ; Science and Technology Commission of Shanghai Municipality[21ZR1475400] ; Science and Technology Commission of Shanghai Municipality[18431907100] ; Program of Shanghai Academic Research Leader[19XD1424600] ; National Science & Technology Major Project Key New Drug Creation and Manufacturing Program, China[2018ZX09711002-006] ; China Postdoctoral Science Foundation[2019M662854]
WOS关键词	(HETERO)ARYL CHLORIDES ; CATALYZED AMINATION ; ARYL CHLORIDES ; CYANATION ; N,N-DIMETHYLFORMAMIDE ; BONDS ; FUNCTIONALIZATION ; ALKYNYLATION ; FORMAMIDES ; AMMONIA
WOS研究方向	Chemistry
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000716793100075
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/298970]
专题	中国科学院上海药物研究所
通讯作者	Dai, Hui-Xiong
作者单位	1.Chinese Acad Sci, Univ Chinese Acad Sci, Shanghai Inst Mat Med, Key Lab Receptor Res, Shanghai 201203, Peoples R China 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 3.Shanghai Univ, Innovat Drug Res Ctr, Dept Chem, Shanghai 200444, Peoples R China
推荐引用方式 GB/T 7714	Cheng, Tai-Jin,Chen, Jun-Jie,Wu, Peng,et al. Copper-Mediated ortho-C-H Amination Using DMF as the Amine Source[J]. ORGANIC LETTERS,2021,23(21):8505-8509.
APA	Cheng, Tai-Jin,Chen, Jun-Jie,Wu, Peng,Xu, Hui,&Dai, Hui-Xiong.(2021).Copper-Mediated ortho-C-H Amination Using DMF as the Amine Source.ORGANIC LETTERS,23(21),8505-8509.
MLA	Cheng, Tai-Jin,et al."Copper-Mediated ortho-C-H Amination Using DMF as the Amine Source".ORGANIC LETTERS 23.21(2021):8505-8509.