364356-63-8Relevant academic research and scientific papers
Insoluble polystyrene-bound bis(oxazoline): Batch and continuous-flow heterogeneous enantioselective glyoxylate-ene reaction
Mandoli, Alessandro,Orlandi, Simonetta,Pini, Dario,Salvadori, Piero
, p. 3233 - 3244 (2007/10/03)
The use of a new, insoluble polymer-bound bis(oxazoline) ligand (IPB-box) for the copper-catalyzed heterogeneous enantioselective glyoxylate-ene reaction is described. Good activity and ee values in the range 85-95% have been obtained during five to seven recycles, either in batch mode or under flow conditions, demonstrating also the recovery and reuse of the whole catalytically active copper complex.
An insoluble polymer-bound bis-oxazoline copper(II) complex: A highly efficient heterogeneous catalyst for the enantioselective Mukaiyama aldol reaction
Orlandi, Simonetta,Mandoli, Alessandro,Pini, Dario,Salvadori, Piero
, p. 2519 - 2521 (2007/10/03)
The polystyrene-supported bis-oxazoline 1 forms a complex with copper(II)triflate that is a highly effective catalyst for the heterogeneously catalyzed enantioselective Mukaiyama aldol reaction of silylthioketene acetals with methyl pyruvate (ca. 90% yiel
Acyl-CoA:cholesterol O-acyltransferase (ACAT) inhibitors. 2. 2-(1,3- dioxan-2-yl)-4,5-diphenyl-1H-imidazoles as potent inhibitors of ACAT
Astles,Ashton,Bridge,Harris,Hart,Parrott,Porter,Riddell,Smith,Williams
, p. 1423 - 1432 (2007/10/03)
The second in this series of papers concerns our further investigations into the search for a potent bioavailable acyl-CoA:cholesterol O- acyltransferase (ACAT) inhibitor suitable for the treatment of atherosclerosis. The design, synthesis, and structure-activity relationship for a series of ACAT inhibitors based on the 2-(1,3-dioxan-2-yl)-4,5- diphenyl-1H-imidazole pharmacophore are described. Compounds such as 13a bearing simple alkyl or hydroxymethyl substituents at the 5-position of the 1,3-dioxane ring are potent bioavailable inhibitors of the rat hepatic microsomal enzyme in vitro (IC50 50 = 10 nM) which contain lipophilic terminal heterocycles do not appear to be systemically available. Less patent but more water soluble compounds such as 13h (IC50 = 60 nM) and 13n (IC50 = 70 nM) are absorbed following oral dosing and achieve plasma levels significantly in excess of their IC50 for ACAT inhibition. These compounds are therefore possible candidates for further investigation as oral antiatherosclerotic agents.
