Sulfoxonium ylides as carbene precursors couple smoothly with thioureas in the presence of 5 mol% of rhodium(II) acetate dimmer via carbenoid insertion to afford the corresponding 2-aminothiazoles with high chemoselectivity, providing a facile and efficient approach to access a variety of 2-aminothiazole derivatives with good functional groups tolerance.
[EN] 4-PHENYL-N-(PHENYL)THIAZOL-2-AMINE DERIVATIVES AND RELATED COMPOUNDS AS ARYL HYDROCARBON RECEPTOR (AHR) AGONISTS FOR THE TREATMENT OF E.G. ANGIOGENESIS IMPLICATED OR INFLAMMATORY DISORDERS<br/>[FR] DÉRIVÉS DE 4-PHÉNYL-N-(PHÉNYL)THIAZOL-2-AMINE ET COMPOSÉS ASSOCIÉS UTILISÉS COMME AGONISTES DU RÉCEPTEUR D'HYDROCARBURE ARYLE (AHR) POUR LE TRAITEMENT, PAR EX., DE TROUBLE LIÉS À L'ANGIOGENÈSE OU INFLAMMATOIRES
申请人:IKENA ONCOLOGY INC
公开号:WO2021127301A1
公开(公告)日:2021-06-24
4-phenyl-N-(phenyl)thiazol-2-amine and 4-(pyridin-3-yl)-N-( phenyl) thiazol-2-amine derivatives and the corresponding thiadiazole, thiophene, oxazole, oxadiazole, imidazole and triazole derivatives and related compounds as aryl hydrocarbon receptor (AHR) agonists for the treatment of angiogenesis implicated disorders, such as e.g. retinopathy, psoriasis, rheumatoid arthritis, obesity and cancer, or inflammatory disorders.
Visible-Light-Mediated Additive-Free Decarboxylative Ketonization Reaction of Acrylic Acids: An Access to α-Thiocyanate Ketones
作者:Zhi-Lv Wang、Jie Chen、Yan-Hong He、Zhi Guan
DOI:10.1021/acs.joc.0c02471
日期:2021.3.5
decarboxylative functionalization of acrylicacids has been developed. The reaction uses inexpensive organic dye 9,10-dicyanoanthracene as a photocatalyst and uses the ubiquitous dioxygen as both an oxygen source and an oxidant. Through this mild and environmentally friendly method, a series of important α-thiocyanate ketones can be generated from easily available acrylicacids and ammonium thiocyanate. In
One-pot synthesis of 4-aryl-2-aminothiazoles from styrenes and thioureas promoted by tribromoisocyanuric acid
作者:Vitor S.C. de Andrade、Marcio C.S. de Mattos
DOI:10.1016/j.tetlet.2020.152164
日期:2020.7
A simple and efficient one-pot protocol has been developed for the conversion of styrenes into 4-aryl-2-aminothiazoles using readily available starting materials. Tribromoisocyanuric acid was successfully used for the co-bromination and oxidation of styrenes to give phenacyl bromides, which in the presence of thioureas produced the corresponding 4-aryl-2-aminothiazoles in 48–70% yield. The protocol