Text for Table of Contents: 6-Indolyldihydropyridinones and 5-indolylmethylenebutyrolactams were prepared from homoallyl amine derivatives resulting the diastereoselective indium-promoted allylation with allyl bromide ethyl 2-(bromomethyl)acrylate, respectively, N-tert-butanesulfinyl imines derived indole-2 3- carbaldehydes.

The majority of phospholipase A2 activity in myocardium is calcium-independent and selective for hydrolysis of plasmalogen substrate (Wolf, R. A., and Gross, R. W. (1985) J. Biol. Chem. 260, 7295-7303; Hazen, S. L., Stuppy, R. J., and Gross, R. W. (1990) J. Biol. Chem. 265, 10622-10630). Accordingly, identification of an inhibitor which selectively targets calcium-independent phospholipases A2 ...

A stereoselective synthesis of the apoptolidin disaccharide is reported. The key chemistry features a new transformation utilizing a highly selective tetramethylalkoxyalanate[v]-directed syn-methylation of a vinylogous ester, isolation of a hydrate of a 2-keto sugar, an eco-friendly radical cleavage of a bromomethyl group, and an efficient preparation of a fluorodisaccharide via the use of Xtal...

Three-step synthesis of 6-amino-2,3-dihydro-4-pyridinones from homoallylamines involving NBS-mediated cyclization of N-(3-butenyl)ureas to 6-(bromomethyl)-2-iminourethanes, dehydrohalogenation and a novel rearrangement as a key step has been developed. The scope and limitations of the method, as well as the mechanism of the rearrangement, supported by kinetic studies and the isolation of N-(1-a...

Phenylboronic acid-modified PEI was prepared by the reaction of 1800 Da PEI with 4-(bromomethyl)phenylboronic acid. It is much more effective than unmodified PEI for gene delivery. The covalently incorporated boronic acid groups achieve the greatly enhanced gene delivery efficiency partially through improving condensation ability to DNA, and partially through facilitating cell uptake due to int...

A highly diastereoselective organocatalytic synthesis of unique functionalised vinyl epoxides, displaying a Morita-Baylis-Hillman backbone, has been developed by means of an user friendly sulfonium ylide epoxidation of aldehydes from a readily available alpha-(bromomethyl)acrylamide derivative. The first result in the asymmetric version is discussed.

In our effort to obtain biologically active compounds, new 3,5-disubstituted 1,3-thiazolidine-2,4diones (5a – r) were synthesized. A series of 5-arylmethylidene-1,3-thiazolidine-2,4-diones (3a – r) were prepared by Knoevenagel reaction from 1,3-thiazolidine-2,4-dione (2) and appropriate aromatic aldehydes. Condensation of 3a – r with 7-hydroxy-4-bromomethyl-2-oxo-2H-chromene (1) afforded novel ...