402567-86-6Relevant articles and documents
Highly efficient and green synthesis of 2,4-diphenyl substituted thiazoles
Zhang, Jungan,Li, Peipei,Zeng, Hongyun,Huang, Yu,Hong, Wei
supporting information, p. 735 - 741 (2020/02/11)
2,4-Diphenyl thiazole is an important organic intermediate and its derivatives contain multiple biological properties. In the present study, we reported a new protocol to synthesize 2,4-diphenyl thiazole analogs, which involved the bromination of ethyl benzoylacetates with NBS in the presence of 2-hydroxypropyl-β-cyclodextrin, followed by a direct cyclization with thiobenzamides in water. Compared with the reported method, the current protocol contains less reaction steps, milder reaction conditions, and simpler workup procedure.
Rhodium(I)-Catalyzed Coupling-Cyclization of C=O Bonds with α-Diazoketones
Chen, Ziyang,Hu, Xinwei,Huang, Junmin,Zeng, Wei
, p. 3980 - 3983 (2018/07/15)
An unprecedented intermolecular nucleophilic attack of C=X bonds (X = O and S) on the rhodium(I)-carbenes has been developed. This transformation allows for the coupling-cyclization of aroylamides with α-diazoketones and provides concise access to 2,4,5-trisubstituted 1,3-oxazoles and 1,3-thiazoles with a broad tolerance of functional groups.
Iron-Catalyzed Synthesis of Substituted Thiazoles from Enamines and Elemental Sulfur through C?S Bond Formation
Wu, Mingzhong,Jiang, Yong,An, Zhenyu,Qi, Zhenjie,Yan, Rulong
, p. 4236 - 4240 (2018/09/20)
An atom economical approach for the synthesis of substituted thiazoles starting from enamines and elemental sulfur through the C?H functionalization/C?S bond formation is described. Under the optimized conditions, various substituted enamines reacted smoothly with elemental sulfur and the desired substituted thiazoles were generated in moderate to excellent yields. (Figure presented.).
Design, synthesis and RON receptor tyrosine kinase inhibitory activity of new head groups analogs of LCRF-0004
Raeppel, Franck,Raeppel, Stéphane L.,Therrien, Eric
, p. 3810 - 3815 (2015/08/24)
New heteroarylcarboxamide head groups substituted with two aromatic rings analogs of thieno[3,2-b]pyridine-based kinase inhibitor LCRF-0004 were designed and synthesized. Potent inhibitors of RON tyrosine kinase with various level of selectivity for c-Met RTK were obtained.
THIAZOLE COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATMENT OF DEGENERATIVE DISEASES AND DISORDERS
-
Paragraph 0071; 0072, (2014/09/30)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.
Discovery of pyrazolthiazoles as novel and potent inhibitors of bacterial gyrase
Ronkin, Steven M.,Badia, Michael,Bellon, Steve,Grillot, Anne-Laure,Gross, Christian H.,Grossman, Trudy H.,Mani, Nagraj,Parsons, Jonathan D.,Stamos, Dean,Trudeau, Martin,Wei, Yunyi,Charifson, Paul S.
scheme or table, p. 2828 - 2831 (2010/08/19)
Bacterial DNA gyrase is an attractive target for the investigation of new antibacterial agents. Inhibitors of the GyrB subunit, which contains the ATP-binding site, are described in this communication. Novel, substituted 5-(1H-pyrazol-3-yl)thiazole compounds were identified as inhibitors of bacterial gyrase. Structure-guided optimization led to greater enzymatic potency and moderate antibacterial potency. Data are presented for the demonstration of selective enzyme inhibition of Escherichia coli GyrB over Staphlococcus aureus GyrB.
Copper(I) bromide-mediated synthesis of novel 2-arylthiazole-5-carboxylates from α-diazo-β-keto esters and aromatic thioamides
Fontrodona,Diaz,Linden,Villalgordo
, p. 2021 - 2027 (2007/10/03)
Starting from readily available α-diazo-β-keto esters 8 and aromatic primary thioamides 9 and 14, a simple synthesis of 2-aryl 4-substituted thiazole-5-carboxylate derivatives of type 10 and 16 has been accomplished. The method is based on the efficient catalysis of CuBr, which promotes the formation of the corresponding carbenoids 11 from diazo derivatives 8. These Cu-carbenoids 11 react with the thiocarbonyl group of the primary thioamides to afford presumably intermediates of the general type 12, which by subsequent cyclocondensation furnish the title thiazole derivatives.
Reactions of tetrasulfur tetranitride antimony pentachloride complex (S4N4 SbCl5) with primary β-enaminones and β-enamino esters: Synthesis of 4-substituted 3-aroyl-and 3-ethoxycarbonyl-1,2,5-thiadiazoles
Bae, Su-Hak,Kim, Kyongtae,Park, Young Ja
, p. 159 - 172 (2007/10/03)
The reaction of tetrasulfur tetranitride antimony pentachloride complex (S4N4·SbCl5) with 3-amino-3-alkyl-1-aryl-2-propenones and 3-amino-1,3- diaryl-2-propenones in toluene at 100°C produced 4-substitued 3-aroyl-1,2,5- th