RESUMEN
Tropic acid was synthesized in a good yield and with high enantioselectivity (81% ee) under non-biphasic conditions via the novel hydrolytic dynamic kinetic resolution of racemic 3-phenyl-2-oxetanone (tropic acid ß-lactone) in the presence of a chiral quaternary ammonium phase-transfer catalyst and strongly basic anion exchange resin as the hydroxide ion donor.
RESUMEN
The synthesis of 3-arylphthalides via palladium-catalyzed arylation of aldehydes with organoboronic acids was achieved using the thioether-imidazolinium carbene ligand in good to excellent yields and was carried out using 1.0 mol % of the catalyst with high substrate tolerance.
Asunto(s)
Aldehídos/química , Benzofuranos/síntesis química , Ácidos Borónicos/química , Hidrocarburos Aromáticos/química , Catálisis , PaladioRESUMEN
Palladium-catalyzed 1,2-addition of potassium aryl- and alkenyltrifluoroborates to aldehydes using thioether-imidazolinium carbene ligands proceeded readily under aqueous conditions. This process tolerated a diverse range of potassium trifluoroborate salts and aldehydes, giving a variety of carbinol derivatives with good to excellent yields.
Asunto(s)
Aldehídos/síntesis química , Boratos/química , Hidrocarburos Cíclicos/química , Imidazolinas/química , Paladio/química , Sulfuros/química , Alquenos/química , Catálisis , Hidrocarburos Fluorados/química , Ligandos , Metano/análogos & derivados , Metano/química , Modelos Químicos , Potasio/química , Soluciones/química , Agua/químicaRESUMEN
The oxindolylidene acetic acids having long N-alkyl chains exhibited strong inhibitory activity toward dual specificity phosphatase Cdc25A.
Asunto(s)
Acetatos/síntesis química , Acetatos/farmacología , Diseño de Fármacos , Indoles/síntesis química , Indoles/farmacología , Fosfatasas cdc25/antagonistas & inhibidores , Acetatos/química , Indoles/química , Isatina/farmacología , Estructura Molecular , Relación Estructura-ActividadRESUMEN
The high level of catalyst performance was attainable in the palladium-catalyzed 1,2-addition of aryl-, heteroaryl-, and alkenylboronic acids to aromatic, heteroaromatic, and aliphatic aldehydes using thioether-imidazolinium chloride L5 as a heterobidentate carbene ligand precursor.
Asunto(s)
Aldehídos/química , Ácidos Borónicos/química , Imidazolinas/química , Paladio/química , Sulfuros/química , Catálisis , Espectroscopía de Resonancia Magnética , Espectrometría de Masa por Ionización de ElectrosprayRESUMEN
[Structure: see text] A novel alicyclic chiral C2-symmetric piperazine, (S,S)-7, is designed and synthesized from L-proline. Benzoylation of a series of cyclic and acyclic meso-1,2-diols with a catalytic amount of (S,S)-7 and CuCl2 provided optically active monobenzoates with high enantioselectivity.
Asunto(s)
Piperazinas/química , Acilación , Diseño de Fármacos , Oxidación-Reducción , EstereoisomerismoRESUMEN
Compounds (6a-e) were synthesized by phosphorylation of hydrophobic perhydroindan derivatives derived from vitamin D(3), and were found to show strong inhibitory activity towards dual-specificity phosphatase Cdc25A (IC(50)=0.7-24.5 microM).
Asunto(s)
Inhibidores Enzimáticos/química , Fosfatos/química , Fosfatasas cdc25/antagonistas & inhibidores , Inhibidores Enzimáticos/síntesis química , Inhibidores Enzimáticos/farmacologíaRESUMEN
Syntheses of D- and L-myo-inositol 3,4,5,6-tetrakisphosphates were achieved via diastereoselective 1,2-addition of vinylcopper reagent with the chiral aldehyde prepared from 1,2,5,6-diisopropylidene-D-glucose, ring-closing metathesis of 1,7-diene with Grubbs catalyst followed by catalytic OsO(4) dihydroxylation of (+)-conduritol B derivatives.
Asunto(s)
Ciclohexanoles/síntesis química , Glucosa/síntesis química , Fosfatos de Inositol/síntesis química , Fosfatos de Inositol/aislamiento & purificación , Ciclohexanoles/metabolismo , Ciclohexenos , Glucosa/metabolismo , Hidroxilación , Fosfatos de Inositol/metabolismo , EstereoisomerismoRESUMEN
Potent dysidiolide analogs were synthesized by structural hybridization of dysidiolide and vitamin D(3). These analogs exhibited strong inhibitory activity toward dual-specificity phosphatase Cdc25A (IC(50)=0.44-0.89 microM).