Formula: C13H18BFO3On October 1, 2019 ,《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》 was published in European Journal of Medicinal Chemistry. The article was written by 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. The article contains the following contents:
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 com. 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] radiolabeled 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. The results came from multiple reactions, including the reaction of (2-Fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)methanol(cas: 1082066-29-2Formula: C13H18BFO3)
(2-Fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)methanol(cas: 1082066-29-2) belongs to organoboron compounds. Organoboron compounds are versatile intermediates and as such are some of the most important classes of reagents in modern organic chemistry. Organoboron compounds are less toxic than organostannane reagents, and unlike alkynylzinc and magnesium, many organoboron compounds possess remarkable oxidative and thermal stabilities. Formula: C13H18BFO3
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