766-81-4Relevant articles and documents
Bis(het)aryl-1,2,3-triazole quinuclidines as α7 nicotinic acetylcholine receptor ligands: Synthesis, structure affinity relationships, agonism activity, [18F]-radiolabeling and PET study in rats
Ouach, Aziz,Vercouillie, Johnny,Bertrand, Emilie,Rodrigues, Nuno,Pin, Frederic,Serriere, Sophie,Boiaryna, Liliana,Chartier, Agnes,Percina, Nathalie,Tangpong, Pakorn,Gulhan, Zuhal,Mothes, Celine,Deloye, Jean-Bernard,Guilloteau, Denis,Page, Guylene,Suzenet, Franck,Buron, Frederic,Chalon, Sylvie,Routier, Sylvain
, p. 449 - 469 (2019/07/03)
In this paper we describe the design and synthesis of bis(Het)Aryl-1,2,3-triazole quinuclidine α7R ligands using an efficient three-step sequence including a Suzuki-Miyaura cross coupling reaction with commercially available and home-made boron derivatives. The exploration of SAR required the preparation of uncommon boron derivatives. Forty final drugs were tested for their ability to bind the target and nine of them exhibited Ki values below nanomolar concentrations. The best scores were always obtained when the 5-phenyl-2-thiophenyl core was attached to the triazole. The selectivity of these compounds towards the nicotinic α4β2 and serotoninergic 5HT3 receptors was assessed and their brain penetration was quantified by the preparation and in vivo evaluation of two [18F] radiolabelled derivatives. It can be expected from our results that some of these compounds will be suitable for further developments and will have effects on cognitive disorders.
COMPOUND FOR ORGANIC OPTOELECTRONIC DEVICE, ORGANIC OPTOELECTRONIC DEVICE AND DISPLAY APPARATUS
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, (2018/12/11)
The present invention relates to a compound for an organic optoelectronic device represented by chemical formula 1, an organic optoelectronic device employing the same and a display device apparatus. The details of chemical formula 1 are as defined in the specification.
Enantioselective synthesis of β-fluoro-β-aryl-α-aminopentenamides by organocatalytic [2,3]-sigmatropic rearrangement
Kasten, Kevin,Slawin, Alexandra M. Z.,Smith, Andrew D.
, p. 5182 - 5185 (2017/11/06)
The tetramisole-promoted catalytic enantioselective [2,3]-sigmatropic rearrangement of quaternary ammonium salts bearing a (Z)-3-fluoro-3-arylprop-2-ene group generates, after addition of benzylamine, a range of β-fluoro-β-aryl-α-aminopentenamides containing a stereogenic tertiary fluorine substituent. Cyclic and acyclic nitrogen substituents as well as various aromatic substituents are tolerated, giving the β-fluoro-β-aryl-α-aminopentenamide products in up to 76% yield, 96:4 dr, and 98:2 er.