3004-59-9Relevant academic research and scientific papers
Palladium-Catalyzed Direct Dicarbonylation of Amines with Ethylene to Imides
Kuai, Chang-Sheng,Wang, Le-Cheng,Xu, Jian-Xing,Wu, Xiao-Feng
supporting information, p. 451 - 456 (2022/01/04)
The selective and effective conversion of low-cost and simple bulk chemicals into high value-added products through catalytic strategy has a wide range of practical significance. Here, a palladium-catalyzed method for the direct and efficient dicarbonylation of amines with basic industrial feedstock ethylene to imide has been developed. Moderate to excellent yields of the desired imides can be produced from readily available amines in a straightforward manner.
Fragment-based design of selective GPCR ligands guided by free energy simulations
Matricon, Pierre,Vo, Duc Duy,Gao, Zhan-Guo,Kihlberg, Jan,Jacobson, Kenneth A.,Carlsson, Jens
supporting information, p. 12305 - 12308 (2021/12/07)
Fragment-based drug discovery relies on successful optimization of weakly binding ligands for affinity and selectivity. Herein, we explored strategies for structure-based evolution of fragments binding to a G protein-coupled receptor. Molecular dynamics s
Synthesis of sulfur heterocycles via domino metal-mediated reactions
Castanheiro, Thomas,Suffert, Jean,Donnard, Morgan,Gulea, Mihaela
, p. 162 - 165 (2017/01/22)
Two methodologies to access S-heterocycles and mixed N,S-heterocycles via metal-mediated domino reactions are described. One involves a cyclocarbopalladation/cross-coupling domino process and leads to benzene-fused five- or six-membered sulfur heterocycles with a stereo defined tetrasubstituted exocyclic double bond. The other consists in a three-component domino reaction between 2-aminophenyl disulfide, copper cyanide, and an electrophile to access N-substituted 2-amino benzothiazoles. Preliminary results in the use of the second method to access N-substituted 2-imino benzothiazoles are also reported.
Aerobic Copper-Mediated Domino Three-Component Approach to 2-Aminobenzothiazole Derivatives
Castanheiro, Thomas,Suffert, Jean,Gulea, Mihaela,Donnard, Morgan
supporting information, p. 2588 - 2591 (2016/06/15)
An unprecedented three-component reaction involving a 2,2′-diaminodiaryl disulfide, copper cyanide, and an electrophile is described. This transformation is based on an oxidative copper-mediated S-cyanation as a key step and involves a cyanation/cyclization/acylation domino sequence enabling a rapid and efficient synthesis of diversely substituted 2-aminobenzothiazole derivatives. Notably, this reaction proceeds via an original mechanism involving an intermolecular migration of the acyl group.
Synthesis, antioxidant properties and radioprotective effects of new benzothiazoles and thiadiazoles
Cressier, Damien,Prouillac, Caroline,Hernandez, Pierre,Amourette, Christine,Diserbo, Michel,Lion, Claude,Rima, Ghassoub
experimental part, p. 5275 - 5284 (2009/12/04)
In this work, we report the synthesis and characterization of new compounds derived from benzothiazoles and thiadiazoles. We observed that structural modifications on these skeletons affected the antioxidant activity. Thiol and aminothiol compounds derived from thiadiazoles and benzothiazoles showed an interesting antioxidant property. The radioprotective activity has also been evaluated in mice. Some of these compounds could be good radioprotectors.
