17852-28-7Relevant academic research and scientific papers
One-Pot Synthesis of 2-Aminobenzophenones from 2-Alkynyl Arylazides Catalyzed by Pd and Cu Precursors
Fan, Hui,Xu, Shijie,Yang, Fan,Zhang, Xiaoxiang,Zhao, Xuechun
supporting information, p. 4555 - 4558 (2021/08/30)
We describe a novel one-pot three-step reaction of 2-alkynyl arylazides through palladium-catalyzed formation of 3-hydroxy-3-phenylindolin-2-ones followed by hydrolysis of amide bonds and copper-catalyzed decarboxylation to give 2-aminobenzophenones. This synthetic method works well with various 2-alkynyl arylazides and affords the products in moderate to good yields under mild reaction conditions.
Lactam Compound, Preparation Method and Use thereof
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Paragraph 0165, (2020/02/14)
Provided is a lactam compound, a tautomer, a stereoisomer, a racemate, a nonequal mixture of enantiomers, a geometric isomer, a solvate, a pharmaceutically acceptable salt thereof, or a solvate of the salt of the compound, and a pharmaceutical composition containing the compound. Also provided are the use of such compounds and their pharmaceutical compositions as drugs, especially as antiviral drugs.
Visible Light Induced Cyclization to Spirobi[indene] Skeletons from Functionalized Alkylidienecyclopropanes
Li, Quanzhe,Liu, Jiaxin,Shi, Min,Wei, Yin
, (2020/03/26)
In this paper, we revealed a metal-free and visible light photoinduced method for the rapid construction of spirobi[indene] skeletons, providing a simple and efficient way for easy access to spirobi[indene] scaffolds under mild conditions along with a broad substrate scope and good functional group tolerance.
Iron-Promoted Construction of Indoles via Intramolecular Oxidative C-N Coupling of 2-Alkenylanilines Using Persulfate
Li, Yudong,Li, Yuehui,Luo, Shuping,Wang, Menglan,Wu, Qing-An
supporting information, p. 3085 - 3090 (2019/08/07)
Indole scaffold synthesis relies primarily on oxidative C-H amination of N-protected alkenylanilines for C-N intramolecular cyclization reactions. Herein, for the first time, without N-protection, various readily prepared 2-alkenylanilines were transformed into the desired indole products in good yields by using K 2 S 2 O 8 as oxidant in the presence of catalytic amounts of FeF 2. The K 2 S 2 O 8 /FeF 2 system offers a direct and benign synthetic route to 3-arylindoles and it is applicable to a wide range of substituted indoles including drug intermediates.
Synthesis of Diiodinated All-Carbon 3,3′-Diphenyl-1,1′-spirobiindene Derivatives via Cascade Enyne Cyclization and Electrophilic Aromatic Substitution
Li, Quanzhe,Yu, Liuzhu,Wei, Yin,Shi, Min
, p. 9282 - 9296 (2019/08/12)
A synthetic method for the construction of diiodinated all-carbon spirobiindene derivatives has been developed from the reaction of propargyl alcohol-tethered alkylidenecyclopropanes with iodine. The reaction proceeded through an iodination-initiated cascade intramolecular enyne cyclization and electrophilic aromatic substitution reaction process in 1,2-dichloroethane upon heating, giving desired spirocyclic products in moderate to excellent yields. Further transformation of the obtained products has also been presented.
Lewis or Br?nsted acid-catalysed reaction of propargylic alcohol-tethered alkylidenecyclopropanes with indoles and pyrroles for the preparation of polycyclic compounds tethered with indole or pyrrole motif
Wei, Hao-Zhao,Yu, Liu-Zhu,Shi, Min
, p. 135 - 139 (2019/12/26)
We developed a facile synthetic method to access cyclopenta[b]naphthalene derivatives via the Lewis or Br?nsted acid catalysed cascade nucleophilic addition, electronic cyclization, ring-opening rearrangement of propargylic alcohol-tethered alkylidenecyclopropanes with indole and pyrrole derivatives. The reaction exhibited a broad substrate scope and good functional group tolerance under metal-free conditions, affording the desired products in moderate to good yields.
HETEROARYL INHIBITORS OF PAD4
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Paragraph 00340-00341, (2018/03/28)
The present invention provides compounds useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.
Chemoselective double annulation of two different isocyanides: Rapid access to trifluoromethylated indole-fused heterocycles
Gao, Yuelei,Hu, Zhongyan,Dong, Jinhuan,Liu, Jun,Xu, Xianxiu
supporting information, p. 5292 - 5295 (2017/11/06)
An unprecedented chemoselective double annulation of α-trifluoromethylated isocyanides with o-acylaryl isocyanides has been developed. This new reaction provides a rapid, efficient, and complete atom-economic strategy for the synthesis of trifluoromethylated oxadiazino[3,2-α]indoles in a single operation from readily available starting materials. Isocyanide insertion into C=O double bonds is disclosed for the first time as indicated by the results of 18O-labeling experiment. A mechanism for this domino reaction is proposed involving chemoselective heterodimerization of two different isocyanides, followed by indole-2,3-epoxide formation and rearrangement.
Method for synthesis of sand smooth biphenyl
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Paragraph 0017; 0018, (2017/03/08)
The invention discloses a synthetic method of 2-cyano-4'-methylbiphenyl, which adopts paratoluidine and benzoyl chloride as raw materials; a Friedel-Crafts acylation reaction is carried out under a Lewis acid catalysis condition; then a ring-closure reaction of a diazonium salt and a benzene ring is carried out in the presence of sodium nitrite; ring opening is carried out under an alkaline condition to generate a main product as shown in formula VI and a byproduct as shown in formula VII, and the ring-opening products are prepared into salts which are then subjected to separation; and finally, carboxyl groups are converted into cyan groups to obtain 2-cyano-4'-methylbiphenyl. The synthetic method of the invention has the advantages of easily available raw materials, safety, convenience for production management, low cost, reduction in 'three wastes' pollution, byproduct recyclability, and improved atom utilization rate.
2-Arylindoles: A new entry to transition metal-free synthesis of 2-aminobenzophenones
Yu, Jin,Moon, Hye Ran,Min, Beom Kyu,Kim, Jae Nyoung
supporting information, p. 893 - 897 (2016/06/14)
Various 2-aminobenzophenones were synthesized from readily available 2-arylindoles in DMSO under O2 balloon atmosphere. The synthesis was carried out without the aid of a transition metal catalyst or moisture-sensitive organometallic reagents from 2-arylindoles.
