59247-63-1Relevant academic research and scientific papers
Synthesis and characterization of novel classes of PDE10A inhibitors - 1H-1,3-benzodiazoles and imidazo[1,2-a]pyrimidines
Moszczyński-P?tkowski, Rafa?,Majer, Jakub,Borkowska, Ma?gorzata,Bojarski, ?ukasz,Janowska, Sylwia,Mat?oka, Miko?aj,Stefaniak, Filip,Smuga, Damian,Bazyd?o, Katarzyna,Dubiel, Krzysztof,Wieczorek, Maciej
, p. 96 - 116 (2018/06/06)
New compounds containing [1,2,4]triazolo [1,5-a]pyridine (I), pyrazolo [1,5-a]pyridine (II), 1H-1,3-benzodiazole (III) and imidazo [1,2-a]pyrimidine (IV) backbones were designed and synthesized for PDE10A interaction. Among these compounds, 1H-1,3-benzodiazoles and imidazo [1,2-a]pyrimidines showed the highest affinity for PDE10A enzyme as well as good metabolic stability. Both classes of compounds were identified as selective and potent PDE10A enzyme inhibitors.
In Situ Preparation and Consumption of O -Mesitylsulfonylhydroxylamine (MSH) in Continuous Flow for the Amination of Pyridines
Brocklehurst, Cara E.,Koch, Guido,Rothe-P?llet, Stephanie,La Vecchia, Luigi
, p. 1636 - 1640 (2017/08/11)
The paper demonstrates a safe method in which highly unstable O -mesitylsulfonylhydroxylamine (MSH) can be prepared and consumed in continuous flow. MSH was prepared in situ and used for the flow amination of a range of pyridines, which were subsequently transformed into useful pyrazolopyridine building blocks.
