Kinetic resolution of racemic C-3 substituted pyrrolidine-2,5-diones has been achieved for the first time using highly efficient oxazaborolidine catalysts derived from cis-1-amino-indan-2-ol.

In the present work, some new 5-[2(3)-dialkylamino alkoxy] Indole 2, 3-diones were prepared from 5-hydroxy isatin. A mixture of 5-hydroxy isatin, dialkylamino alkylhalide in alcoholic potassium hydroxide was stirred at room temperature for 6 hours to get the 5-[2(3)dialkylamino alkoxy] Indole 2,3-diones. The structures of the products were characterized by IR, NMR, MASS Spectral studies. All th...

A facile one-pot benzannulation strategy involving phosphine-3-alkyl allenoate zwitterions and cyclic 1,2-diones is described. The strategy is effectively utilized in the synthesis of fluoranthenes and benzo[a]aceanthrylenes with impressive photophysical properties. This is the first report on an intermolecular benzannulation using a 3-alkyl allenoate as a four carbon synthon.

Abstract. The Ti(OiPr)4/tartaric acid diethyl ester/t-BuOOH complex (Sharpless catalyst) was successfully used for the direct asymmetric oxidation of ketones resulting in lactones from cyclobutanones; α,β-dihydroxy ketones from β-hydroxy ketones; alkyl lactone carboxylic acids from 3-alkylcyclopentane-1,2-diones; and spiro-γ-dilactone from 3-(2-hydroxyethyl)cyclopentane1,2-dione in high enantio...

We have developed an organocatalyzed three-component reaction of 1,2-diones, aldehydes and arylamines, which provides an efficient approach to access polysubstituted pyrroles. In the catalysis of 4-methylbenzenesulfonic acid monohydrate, the reactions of a wide range of 1,2-diones, arylamines and aldehydes took place smoothly to generate the corresponding polysubstituted pyrroles in acceptable ...

The study presented here is a follow up of the authors' interest in the approach to selective and cytotoxic bioreductive anticancer prodrugs. The current work is devoted to explore both the biological activity of some previously obtained compounds and the search for an explanation of their target(s) in hypoxic pathways. In this work the biological activity of some benzimidazole-4,7-diones was e...

The synthesis of the title compounds was carried out by reacting dicarboxylic acid chlorides with oximes in the presence of excess triethylamine. Disubstituted malonyl chlorides gave 2-alkenyl-4,4-dialkyl-3,5-isoxazolidinediones (8a-f) and 2,2'-ethylidene-bis[4,4-dialkyl-3,5-isoxazolidinedione]s (9a-f). Compounds 9 were formed from 8 and its N-unsubstituted 3,5-isoxazolidinedione decomposition ...

The synthesis of 2,5-disubstituted 5,6-dihydro-lH-pyrido[l,2-a]quinazoline-l,6-diones (3) by reacting monosubstituted bis 2,4,6-trichlorophenyl malonates (1) with 3-aryl-3,4dihydro-2-methyl-4-quinazolinones (2) is described. Allylation of the pyridoquinazoline 3 c with allylbromide afforded the corresponding 3-allyloxy derivative 4. Certain generalizations of the cleavage processes of this seri...

For the first time, a catalytic asymmetric Henry reaction of 1H-pyrrole-2,3-diones was achieved with a chiral bifunctional amine-thiourea as a catalyst possessing multiple hydrogen-bond donors. With this developed method, a range of 3-hydroxy-3-nitromethyl-1H-pyrrol-2(3H)-ones bearing quaternary stereocenters were obtained in acceptable yield (up to 75%) and enantioselectivity (up to 73% ee).

Several small-molecule CDK inhibitors have been identified, but none have been approved for clinical use in the past few years. A new series of 4-[(3-hydroxybenzylamino)-methylene]-4H-isoquinoline-1,3-diones were reported as highly potent and selective CDK4 inhibitors. In order to find more potent CDK4 inhibitors, the interactions between these novel isoquinoline-1,3-diones and cyclin-dependent...