93020-55-4Relevant articles and documents
α-Selective C(sp3)-H Thio/Selenocyanation of Ketones with Elemental Chalcogen
Li, Jin-Cheng,Gao, Wen-Xia,Liu, Miao-Chang,Zhou, Yun-Bing,Wu, Hua-Yue
, p. 17294 - 17306 (2021/12/02)
A facile method is disclosed for the synthesis of α-thio/selenocyanato ketones through regioselective C-H thio/selenocyanation of ketones. The advantages include the use of easily available starting materials, high efficiency, simple operation, and easy scale-up. Control experiments provide evidence that the reaction proceeded via a radical way, while kinetic isotope effect experiments reveal that the cleavage of the C-H bond serves as the rate-limiting step.
Highly efficient heterogeneous copper-catalysed coupling of oxime acetates with isothiocyanates leading to 2-aminothiazoles
Tuo, Yuxink,Yao, Fang,Liao, Yang,Cai, Mingzhong
, p. 225 - 229 (2017/06/20)
The heterogeneous coupling reaction of oxime acetates with isothiocyanates was achieved at 110°C in toluene in air in the presence of a bidentate nitrogen-functionalised MCM-41-immobilised copper(I) complex (MCM-41-2N-CuI) with Cs2CO3 as base to afford a variety of 2-aminothiazoles in good yields. The MCM-41-2N-CuI catalyst can be easily recovered by a simple filtration and reused at least eight times without significant loss of activity.
Substituted 2-aminothiazoles are exceptional inhibitors of neuronal degeneration in tau-driven models of Alzheimer's disease
Lagoja, Irene,Pannecouque, Christophe,Griffioen, Gerard,Wera, Stefaan,Rojasdelaparra, Veronica Maria,Van Aerschot, Arthur
, p. 386 - 392 (2012/05/31)
A novel series of 2-aminothiazoles with strong protection in an Alzheimer's disease (AD) model comprising tau-induced neuronal toxicity is disclosed. These derivatives can be synthesized in one-pot and a small SAR of the substitution within these series afforded several compounds that counteracted tau-induced cell toxicity at nanomolar concentrations. These congeners therefore have strong potential as possible treatment for Alzheimer's disease and other related tauopathies.