156146-13-3Relevant articles and documents
The Diverse Reactivity of Homopropargylic Amines as “Masked” 1C Synthons for the Aza-Friedel–Crafts Alkylation of Indoles
Chen, Hao,Ni, Min,Bao, Xiaofeng,Wang, Chan,Liu, Lingyan,Chang, Weixing,Li, Jing
, p. 470 - 476 (2018)
A novel type of “masked” 1C synthon was developed through the hydroamination cyclization-protonation of homopropargylic amines to act as aza-Friedel–Crafts alkylation reagents to react with indoles. A variety of 3-(2-pyrrolidinyl)indoles were generated in good to high yields. More significantly, some of the corresponding products display potential bioactivity against chlamydial infection, wherein they specifically target the mid-stage of the chlamydial life cycle by interfering with RB replication.
Metal-free, redox-neutral, site-selective access to heteroarylamine via direct radical?radical cross-coupling powered by visible light photocatalysis
Zhou, Chao,Lei, Tao,Wei, Xiang-Zhu,Ye, Chen,Liu, Zan,Chen, Bin,Tung, Chen-Ho,Wu, Li-Zhu
supporting information, p. 16805 - 16813 (2020/11/09)
Transition-metal-catalyzed C?N bond-forming reactions have emerged as fundamental and powerful tools to construct arylamines, a common structure found in drug agents, natural products, and fine chemicals. Reported herein is an alternative access to heteroarylamine via radical?radical cross-coupling pathway, powered by visible light catalysis without any aid of external oxidant and reductant. Only by visible light irradiation of a photocatalyst, such as a metal-free photocatalyst, does the cascade single-electron transfer event for amines and heteroaryl nitriles occur, demonstrated by steady-state and transient spectroscopic studies, resulting in an amine radical cation and aryl radical anion in situ for C?N bond formation. The metal-free and redox economic nature, high efficiency, and site-selectivity of C?N cross-coupling of a range of available amines, hydroxylamines, and hydrazines with heteroaryl nitriles make this protocol promising in both academic and industrial settings.
HETEROCYCLIC COMPOUNDS AS RSV INHIBITORS
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Paragraph 0455-0456, (2019/01/15)
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.