Catalytic asymmetric formal [3+2] cycloaddition of isatogens with azlactones to construct indolin-3-one derivatives
The chiral amide-guanidine-catalyzed asymmetric formal [3+2] cycloaddition of isatogens with azlactones is presented. This strategy provided a facile and feasible route to chiral indolin-3-one derivatives bearing two contiguous tetrasubstituted stereocent
A cascade approach to 3D cyclic carbamates: Via an ionic decarboxylative functionalization of olefinic oxamic acids
An m-CPBA-mediated intramolecular epoxidation-decarboxylative alkoxylation cascade reaction of olefinic oxamic acids has been developed. The distinct ionic decarboxylative mechanism was preliminarily revealed. The protocol features mild reaction conditions and operational simplicity, allowing the construction of diverse medicinally valuable 5-7 membered 3D cyclic carbamate architectures in moderate to high yields.
Palladium-catalyzed cross-coupling of aryl chlorides with alkenylboronic acids with low E/Z isomerization
Using a bulky electron-rich monodentate benzoferrocenyl phosphine as supporting ligand, an efficient protocol for stereoselective palladium-catalyzed Suzuki-Miyaura cross-coupling of aryl chlorides with alkenylboronic acids was uncovered. Using this protocol, both trans- and cis-alkenylboronic acids can be coupled with high stereoselectivity giving the corresponding vinylarenes in good to quantitative yields. Electron-poor and -rich aryl chlorides including highly hindered ones are all suitable substrates for the reaction.
Thimmaiah, Muralidhara,Zhang, Xiang,Fang, Shiyue
p. 5605 - 5607
(2008/12/22)
Structural development of liver X receptor (LXR) antagonists derived from thalidomide-related glucosidase inhibitors
Following our previous discovery of LXR antagonistic activity of 2′-substituted phenylphthalimides derived from thalidomide-related glucosidase inhibitors, structure-activity studies and further structural development led to 5-chloro-N-2′-n-pentylphenyl-1,3-dithiophthalimide (5CPPSS-50), with IC50 values of about 10 and 13 μM for LXRα and LXR β, respectively.