The organocatalytic ring-opening of N-tosyl protected aziridines by beta-ketoesters under chiral PTC-conditions, leading to the formation of optically active aminoethyl functionalised compounds with up to 99% ee, has been developed.

The development of new and efficient methods, reagents, catalysts for the introduction fluorine atoms or fluorinated moieties in molecular scaffolds has become a topic paramount importance organic synthesis. In this framework, incorporation SCF3 group into molecule often led to beneficial effects on drug’s metabolic stability bioavailability. Here we report our studies aimed stereoselective syn...

BACKGROUND Based on the pharmacological potency and structural features of succinimides, this study was designed to synthesize new ketoesters derivatives of succinimides. Furthermore, the synthesized compounds were evaluated for their possible anticholinesterase and antioxidant potentials. The compounds were synthesized by organocatalytic Michael additions of α-ketoesters to N-aryl maleimides. ...

A facile synthesis of 2,3-dihydropyrrole derivatives has been achieved through the one-pot, three-component tandem reaction of diazo compounds with anilines and beta,gamma-unsaturated alpha-ketoesters in moderate to good yields.

The first organocatalytic "anti-Michael" reaction of cyclic-beta-ketoesters to unsaturated double bonds is described in a highly asymmetric version leading to the synthesis of alpha,alpha'-disubstituted branched double bonds as optically active Baylis-Hillman-like adducts.

A gene encoding an NADH-dependent short-chain dehydrogenase/reductase (gox2036) from Gluconobacter oxydans 621H was cloned and heterogeneously expressed in Escherichia coli. The protein (Gox2036) was purified to homogeneity and biochemically characterized. Gox2036 was a homotetramer with a subunit size of approximately 28 kDa. Gox2036 had a strict requirement for NAD⁺/NADH as the cofactor. Gox2...

The palladium-catalyzed reaction of (hetero)aryl bromides, chlorides, and nonaflates with α-allyl-β-ketoesters provides ready efficient access to functionalized 2,3-dihydrofurans. The reaction tolerates several useful substituents including chloro, fluoro, ether, ketone, ester, cyano, and nitro groups.

β-Isocupreidine (β-ICD) catalyzed asymmetric [4 + 2] cycloaddition of β,γ-unsaturated α-ketoesters with allenic esters afforded ester-substituted functionalized dihydropyran derivatives in high yields along with high enantioselectivities under mild conditions.

The proton catalyzed reaction of methyldiazoacetate and benzaldehyde resulting in the formation of b-ketoesters and 3-hydroxyacrylates has been investigated by means of DFT/B3LYP calculations. Experimentally this reaction is performed using HBF4 Et2O as the catalyst and CH2Cl2 as the solvent. Several mechanistic pathways involving 1,2-migration of phenyl-, H-, and OH-substituents have been cons...

It has been shown for the first time that relatively electron deficient triazolium pre-catalysts promote (at low loadings in the presence of base) highly chemoselective crossed acyloin condensation reactions between aldehydes and a-ketoesters to afford densely functionalized products incorporating a quaternary stereocentre of considerable synthetic potential. Hydroacylation pathways which have ...