14 research outputs found
Les sels d'onium à tâche spécifique (nouveaux supports (hydro-) solubles pour la synthèse organique)
No full textCe travail présente l'utilisation des liquides ioniques et de sels d'onium à tâche spécifique comme supports (hydro) solubles pour la synthèse organique supportée. après un préliminaire sur la synthèse organique supportée et un rappel sur la chimie des liquides ioniques, des sels d'onium à tâche spécifique ont été utilisés comme support soluble pour la réaction de baylis-hillman. Sont présentées ensuite la synthèse de sels d'onium à tâche spécifique et leur utilisation comme supports solubles en milieu aqueux, un acrylamide greffé sur un sel d'ammonium pour la réaction de michael et de heck et un aldéhyde supporté sur un chlorure d'ammonium pour la synthèse de tétrahydroquinoléines et de quinoléines ainsi que la réaction multi-composants de UGI. Au cours de ce travail, l accent est mis sur la possibilité de moduler les propriétés du sel d'onium à tâche spécifique en fonction des caractéristiques de stabilité et de solubilité souhaitées.RENNES1-BU Sciences Philo (352382102) / SudocSudocFranceF
ChemInform Abstract: Onium Salt Supported Organic Synthesis in Water: Application to Ugi′s 4‐Components Reaction.
No full textChemInform Abstract: Onium Salt Supported Organic Synthesis in Water: Application to Grieco′s Multicomponent Reaction.
No full textChemInform Abstract: Efficient Synthesis of the First N-Methyloxoarcyriaflavin Including and Original Central Seven-Membered Cycle.
No full textAchieving Chemo-, Regio-, and Stereoselectivity in Palladium-Catalyzed Reaction of γ-Borylated Allylic Acetates
No full textThree-carbon highly functionalized γ-borylated allylic acetates underwent a regio- and stereocontrolled Tsuji–Trost reaction in the presence of palladium complexes. An ipso substitution of the acetate with complete stereoretention of the chiral center was achieved, leading to vinylic boronates with enantiomeric excesses above 99%
Achieving Chemo-, Regio-, and Stereoselectivity in Palladium-Catalyzed Reaction of γ-Borylated Allylic Acetates
No full textChemInform Abstract: Achieving Chemo-, Regio-, and Stereoselectivity in Palladium-Catalyzed Reaction of γ-Borylated Allylic Acetates.
No full textEfficient Synthesis of the First N-Methyloxoarcyriaflavin Including an Original Central Seven-Membered Cycle
No full textInternational audienc
Advances in tetrahydropyrido[1,2-a]isoindolone (valmerins) series: Potent glycogen synthase kinase 3 and cyclin dependent kinase 5 inhibitors.
No full textInternational audienceAn efficient synthetic strategy was developed to modulate the structure of the tetrahydropyridine isoindolone (Valmerin) skeleton. A library of more than 30 novel final structures was generated. Biological activities on CDK5 and GSK3 as well as cellular effects on cancer cell lines were measured for each novel compound. Additionally docking studies were performed to support medicinal chemistry efforts. A strong GSK3/CDK5 dual inhibitor (38, IC50 GSK3/CDK5 32/84 nM) was obtained. A set of highly selective GSK3 inhibitors was synthesized by fine-tuning structural modifications (29 IC50 GSK3/CDK5 32/320 nM). Antiproliferative effects on cells were correlated with the in vitro kinase activities and the best effects were obtained with lung and colon cell lines
Design of 7 nicotinic acetylcholine receptor ligands in quinuclidine, tropane and quinazoline series. Chemistry, molecular modeling, radiochemistry, in vitro and in rats evaluations of a [F] quinuclidine derivative
No full textInternational audienceIn this report, we describe the synthesis of a novel library of 7 nAChR ligands based on the modulationof the quinuclidine, quinazoline and tropane moieties. Spirane derivatives were newly synthesized understereo specific 1,3 dipolar cylcoadditions. Only amide derivatives bonded efficiently to the receptor withKi measured between 14 and 133 nM. The best fluorinated candidate was selected and radiolabeled. Thepotent [F]4 PET tracer was evaluated in rats and its brain accumulation quantified
