Decatungstodivanadogermanic acid (H6GeW10V2O40.22H2O) was used as a green heterogeneous catalyst for the synthesis of 3,4-dihydropyrimidin-2-(1H)-ones from one-pot three-component cyclocondensation reaction of a β-ketoester, an aldehyde and urea/thiourea under solvent-free conditions is reported. This method provides an efficient and much improved modification of the original Biginelli reaction...

Decatungstodivanadogermanic acid (H6GeW10V2O40.22H2O) was used as a green heterogeneous catalyst for the synthesis of 3,4-dihydropyrimidin-2-(1H)-ones from one-pot three-component cyclocondensation reaction of a β-ketoester, an aldehyde and urea/thiourea under solvent-free conditions is reported. This method provides an efficient and much improved modification of the original Biginelli reaction...

An efficient protocol for the synthesis of 3,4-dihydropyrimidin-2-(1H)-one/thione derivatives via multi-component coupling reaction of aromatic aldehydes, β-ketoester and urea or thiourea under solvent-free conditions using Silica Supported Barium Chloride as a catalyst is described. All prepared compounds with melting points, IR,1H NMR and 13C NMR were identified. High yields, mild conditi...

Synthesis of cyclopenta[b]pyrane derivatives via Achmatowicz oxidative cyclization of furanols followed by intramolecular Knoevenagel condensation of the β-ketoester arm is examined. The extent of diastereoselectivity was dependent on the nature of the chiral atom within the tethering carbon of the pyrenone ring. In some cases, this process proceeds with a high degree of stereoselectivity after...

The title compound, C17H24O5, featuring a 2-carbeth-oxy-3-oxepanone unit in its intra-molecularly O-H⋯O hydrogen-bonded enol form, was obtained via [(CF3CO2)2Rh]2-catal-ysed intra-molecular O-H bond insertion in the α-diazo-ω-hy-droxy-β-ketoester, ethyl 4-[(1S,3aS,6R,6aS)-6-hy-droxy-2,2,3a-trimethyl-3-oxo-octa-hydro-penta-len-1-yl]-2-diazo-3-oxobutano-ate. The seven-membered oxacyclic ring, thu...

This study presents the bioreduction of six β-ketoesters by whole cells of Kluyveromyces marxianus and molecular investigation of a series of 13 β-ketoesters by hologram quantitative structure-activity relationship (HQSAR) in order to relate with conversion and enantiomeric excess of β-stereogenic-hydroxyesters obtained by the same methodology. Four of these were obtained as (R)-configuration a...

A divergent asymmetric total synthesis of voacafricines and B, hexacyclic monoterpene indole alkaloids, has been accomplished featuring the following key steps: a) a catalyst-controlled Pictet–Spengler reaction 6-methoxytryptamine with chiral α-ketoester affording 1,1-disubstituted tetrahydro-β-carboline in excellent yield diastereoselectivity; b) oxidative cleavage 3,5-disubstituted cyclopente...

Abstract Fluoroquinolones such as levofloxacin and ciprofloxacin are potent antibiotics prescribed to treat various bacterial infections. Recent studies have also identified prominent examples promising anti‐cancer agents. However, significant off‐target effects observed in human patients precluded their wide‐spread clinical use. For instance, upon systemic administration, overt toxicity toward...