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.
Chiral Benzothiophene Synthesis via Enantiospecific Coupling of Benzothiophene S-Oxides with Boronic Esters
Aggarwal, Varinder K.,Noble, Adam,Sang, Ruocheng
supporting information, p. 25313 - 25317 (2021/11/09)
Benzothiophenes are valuable heterocycles that are widely used in medicines, agrochemicals, and materials science. Herein, we report a general method for the synthesis of enantioenriched 2,3-disubstituted benzothiophenes via a transition-metal-free C2-alkylation of benzothiophenes with boronic esters. The reactions utilize benzothiophene S-oxides in lithiation-borylations to generate intermediate arylboronate complexes, and subsequent Tf2O-promoted S?O bond cleavage to trigger a Pummerer-type 1,2-metalate shift, which gives the coupled products with complete enantiospecificity. Primary, secondary and tertiary alkyl boronic esters and aryl boronic esters are successfully coupled with a range of C3-substituted benzothiophenes. Importantly, this transformation does not require the use of C3 directing groups, therefore it overcomes a major limitation of previously developed transition-metal-mediated C2 alkylations of benzothiophenes.
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.
