title: Silver-catalysed direct amination of unactivated C-H bonds of functionalized molecules.
abstract: Carbon-nitrogen bond formation from inert C-H bonds is an ideal organic transformation and a highly desirable method for the synthesis of N-containing molecules due to its high efficiency and atom economy. In this report, we develop a general reaction to achieve an unprecedented selective intramolecular amination of unactivated C-H bond in the absence of complex directing groups. Functionalized heterocyclic products are built up from readily available linear amines through simple and reliable silver catalysis, representing a new silver-based C-H functionalization. This method displays preference for primary sp(3) C-H bonds and exhibits distinct chemo- and regioselectivity compared to existing methods of direct amination (Hofmann-Löffler-Freytag reaction and nitrene insertion). The study highlights the manipulation of unfunctionalized groups in organic molecules to furnish complex structural units in the natural and bioactive molecules.
authors.affiliation: Beijing National Laboratory of Molecular Sciences (BNLMS) and Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Green Chemistry Center, Peking University, Beijing 100871, China.
authors.forename: Mingyu
authors.initials: M
authors.lastname: Yang
authors.affiliation: Beijing National Laboratory of Molecular Sciences (BNLMS) and Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Green Chemistry Center, Peking University, Beijing 100871, China.
authors.forename: Bo
authors.initials: B
authors.lastname: Su
authors.affiliation: Beijing National Laboratory of Molecular Sciences (BNLMS) and Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Green Chemistry Center, Peking University, Beijing 100871, China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Wang
authors.affiliation: Beijing National Laboratory of Molecular Sciences (BNLMS) and Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Green Chemistry Center, Peking University, Beijing 100871, China.
authors.forename: Kang
authors.initials: K
authors.lastname: Chen
authors.affiliation: Beijing National Laboratory of Molecular Sciences (BNLMS) and Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Green Chemistry Center, Peking University, Beijing 100871, China.
authors.forename: Xingyu
authors.initials: X
authors.lastname: Jiang
authors.affiliation: Beijing National Laboratory of Molecular Sciences (BNLMS) and Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Green Chemistry Center, Peking University, Beijing 100871, China.
authors.forename: Yun-Fei
authors.initials: YF
authors.lastname: Zhang
authors.affiliation: Beijing National Laboratory of Molecular Sciences (BNLMS) and Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Green Chemistry Center, Peking University, Beijing 100871, China.
authors.forename: Xi-Sha
authors.initials: XS
authors.lastname: Zhang
authors.affiliation: Beijing National Laboratory of Molecular Sciences (BNLMS) and Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Green Chemistry Center, Peking University, Beijing 100871, China.
authors.forename: Guihua
authors.initials: G
authors.lastname: Chen
authors.affiliation: Beijing National Laboratory of Molecular Sciences (BNLMS) and Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Green Chemistry Center, Peking University, Beijing 100871, China.
authors.forename: Ye
authors.initials: Y
authors.lastname: Cheng
authors.affiliation: Beijing National Laboratory of Molecular Sciences (BNLMS) and Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Green Chemistry Center, Peking University, Beijing 100871, China.
authors.forename: Zhichao
authors.initials: Z
authors.lastname: Cao
authors.affiliation: Beijing National Laboratory of Molecular Sciences (BNLMS) and Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Green Chemistry Center, Peking University, Beijing 100871, China.
authors.forename: Qing-Yun
authors.initials: QY
authors.lastname: Guo
authors.affiliation: Shenzhen Graduate School of Peking University, Shenzhen 518055, China.
authors.forename: Lushun
authors.initials: L
authors.lastname: Wang
authors.affiliation: 1] Beijing National Laboratory of Molecular Sciences (BNLMS) and Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, College of Chemistry and Green Chemistry Center, Peking University, Beijing 100871, China [2] State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, China [3] State Key Laboratory of Organometallic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China.
authors.forename: Zhang-Jie
authors.initials: ZJ
authors.lastname: Shi