1455-18-1Relevant articles and documents
An Efficient One-Pot Method for the Preparation of Polysubstituted Benzothiophenes
Buchwald, Stephen L.,Fang, Qun
, p. 2793 - 2797 (1989)
A one-pot method for the transformation of an aryl bromide, an internal alkyne, and sulfur dichloride into a polysubstituted benzothiophene, in high yield, is described.The method involves the generation and trapping of a zirconocene complex of a substituted benzyne.
Nickel-Catalyzed Asymmetric Hydrogenation of Cyclic Alkenyl Sulfones, Benzo[ b]thiophene 1,1-Dioxides, with Mechanistic Studies
Liu, Gongyi,Tian, Kui,Li, Chenzong,You, Cai,Tan, Xuefeng,Zhang, Heng,Zhang, Xumu,Dong, Xiu-Qin
supporting information, p. 668 - 675 (2021/02/06)
A highly efficient catalytic system based on the cheap transition metal nickel for the asymmetric hydrogenation of challenging cyclic alkenyl sulfones, 3-substituted benzo[b]thiophene 1,1-dioxides, was first successfully developed. A series of hydrogenation products, chiral 2,3-dihydrobenzo[b]thiophene 1,1-dioxides, were obtained in high yields (95-99%) with excellent enantioselectivities (90-99% ee). According to the results of nonlinear effect studies, deuterium-labeling experiments, and DFT calculation investigations, a reasonable catalytic mechanism for this nickel-catalyzed asymmetric hydrogenation was provided, which displayed that the two added hydrogen atoms of the hydrogenation products could be from H2 through the insertion of Ni-H and subsequent hydrogenolysis.
Thiophene compounds and applications of thiophene compounds serving as USP7 inhibitors and antitumor drugs
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Paragraph 0066; 0070; 0071, (2019/01/16)
The invention discloses compounds shown in the formula I or nitrogen oxides, pharmaceutically acceptable salt or solvate of the compounds, a preparation method of the compounds, and applications of the compounds in pharmacy, and particularly provides the applications of the compounds serving as USP7 inhibitors and antitumor drugs. Pharmacodynamic experiment results show that the compounds in the formula I have inhibition effects on a USP7 enzyme and also have proliferation inhibition effects on human colon cancer cells HCT-116. Therefore, the compounds can be used for preparing the drugs for preventing or treating diseases related to tumors. The formula I is shown in the description.
A simple protocol for Cu-catalyzed protodecarboxylation of (hetero)aromatic carboxylic acids
Li, Zhaojie,Fu, Zhengjiang,Zhang, Haixia,Long, Jiao,Song, Yuanyuan,Cai, Hu
supporting information, p. 3014 - 3018 (2016/05/09)
A simple and practical protodecarboxylation of o-nitrobenzoic acids as well as heteroaromatic carboxylic acids with various substituents via using CuI/Et3N has been established. This transformation provides a viable and low-cost approach to generating previously unavailable substituted arenes from readily accessible aryl carboxylic acids as the starting materials.