61109-48-6Relevant articles and documents
Pd-catalyzed allylative dearomatisation using Grignard reagents
Boldrini, Cosimo,Harutyunyan, Syuzanna R.
supporting information, p. 11807 - 11810 (2021/11/30)
Pd-catalyzed allylative dearomatisation of naphthyl halides is shown to be feasible by employing Grignard reagents. The high reactivity of the nucleophile allows for fast reactions and low catalyst loading, while a plethora of successfully substituted compounds illustrate the broad scope. Five membered heteroaromatic compounds are also demonstrated to be reactive under similar conditions.
Development of new highly potent imidazo[1,2-b[pyridazines targeting Toxoplasma gondii calcium-dependent protein kinase 1
Moine, Espérance,Dimier-Poisson, Isabelle,Enguehard-Gueiffier, Cécile,Logé, Cédric,Pénichon, Mélanie,Moiré, Nathalie,Delehouzé, Claire,Foll-Josselin, Beátrice,Ruchaud, Sandrine,Bach, Stéphane,Gueiffier, Alain,Debierre-Grockiego, Fran?oise,Denevault-Sabourin, Caroline
, p. 80 - 105 (2015/11/02)
Using a structure-based design approach, we have developed a new series of imidazo[1,2-b]pyridazines, targeting the calcium-dependent protein kinase-1 (CDPK1) from Toxoplasma gondii. Twenty derivatives were thus synthesized. Structure-activity relationships and docking studies confirmed the binding mode of these inhibitors within the ATP binding pocket of TgCDPK1. Two lead compounds (16a and 16f) were then identified, which were able to block TgCDPK1 enzymatic activity at low nanomolar concentrations, with a good selectivity profile against a panel of mammalian kinases. The potential of these inhibitors was confirmed in vitro on T. gondii growth, with EC50 values of 100 nM and 70 nM, respectively. These best candidates also displayed low toxicity to mammalian cells and were selected for further in vivo investigations on murine model of acute toxoplasmosis.
Asymmetric transfer hydrogenation of 1-naphthyl ketones by an ansa-Ru(II) complex of a DPEN-SO2N(Me)-(CH2)2(η 6-p-tol) combined ligand
Kisic, Andrea,Stephan, Michel,Mohar, Barbara
supporting information, p. 1614 - 1617 (2013/06/26)
The first second-generation designer Ru(II) catalyst 1b featuring an enantiopure N,C-(N-ethylene-N-methyl-sulfamoyl)-tethered (DPEN- κ2N,N′)/η6-toluene hybrid ligand is introduced. Using an S/C = 1000 in HCO2H-Et3N 5:2 transfer hydrogenation medium, secondary 1-naphthyl alcohols are obtained in up to >99.9% ee under mild conditions. Mechanistic factors are discussed.
