17847-35-7Relevant articles and documents
Zirconium-hydride-catalyzed site-selective hydroboration of amides for the synthesis of amines: Mechanism, scope, and application
Han, Bo,Jiao, Haijun,Wu, Lipeng,Zhang, Jiong
, p. 2059 - 2067 (2021/09/02)
Developing mild and efficient catalytic methods for the selective synthesis of amines is a longstanding research objective. In this respect, catalytic deoxygenative amide reduction has proven to be promising but challenging, as this approach necessitates selective C–O bond cleavage. Herein, we report the selective hydroboration of primary, secondary, and tertiary amides at room temperature catalyzed by an earth-abundant-metal catalyst, Zr-H, for accessing diverse amines. Various readily reducible functional groups, such as esters, alkynes, and alkenes, were well tolerated. Furthermore, the methodology was extended to the synthesis of bio- and drug-derived amines. Detailed mechanistic studies revealed a reaction pathway entailing aldehyde and amido complex formation via an unusual C–N bond cleavage-reformation process, followed by C–O bond cleavage.
First Nondiscriminating Translocator Protein Ligands Produced from a Carbazole Scaffold
Cheng, Hei Wun Alison,Sokias, Renee,Werry, Eryn L.,Ittner, Lars M.,Reekie, Tristan A.,Du, Jonathan,Gao, Quanqing,Hibbs, David E.,Kassiou, Michael
supporting information, p. 8235 - 8248 (2019/10/11)
Development of neuroinflammation agents targeting the translocator protein (TSPO) has been hindered by a common single nucleotide polymorphism (A147T) at which TSPO ligands commonly lose affinity. To this end, carbazole acetamide scaffolds were synthesized and structure activity relationships elaborated to explore the requirements for high-affinity binding to both TSPO wild type (WT) and the polymorphic TSPO A147T. This study reports high binding affinity and nondiscriminating TSPO ligands.
Exploiting the 4-Phenylquinazoline Scaffold for the Development of High Affinity Fluorescent Probes for the Translocator Protein (TSPO)
Milite, Ciro,Barresi, Elisabetta,Da Pozzo, Eleonora,Costa, Barbara,Viviano, Monica,Porta, Amalia,Messere, Anna,Sbardella, Gianluca,Da Settimo, Federico,Novellino, Ettore,Cosconati, Sandro,Castellano, Sabrina,Taliani, Sabrina,Martini, Claudia
, p. 7897 - 7909 (2017/10/06)
The quinazoline class was exploited to search for a new translocator protein (TSPO) fluorescent probe endowed with improved affinity and residence time (RT). Computational studies on an "in-house" collection of quinazoline derivatives, featuring highly st