2,4-Diketo esters: Crucial intermediates for drug discovery

Synthesis, characterization, antitumor potential, and investigation of mechanism of action of copper(ii) complexes with acylpyruvates as ligands: interactions with biomolecules and kinetic study

“…Numerous studies have been conducted with different strategies. [11][12][13][14][15] One of the most important is the replacement of platinum metal ions with some other metal that shows less toxicity or, in an even better case, with some essential metal. [16][17][18] Keeping in mind the previous and knowing that copper is an essential element with numerous biological functions in the human organism, as well as our previous experiences with copper compounds, we came up with the idea to examine the antitumor potential of a series of copper(II) complexes.…”

Synthesis, recyclization under the action of methanol and analgetic activity of N'-(5-aryl-2-oxofuran-3(2H)-ylidene)furan-2-carbohydrazides

“…Such a universal structural fragment can be found among the 3-imino-(hydrazinylidene)-furan-2(3H)-one derivatives, which results from their chemical availability due to the scalability of the synthetic methods [8] and the reactivity [9][10][11][12][13][14][15]. For example, the reactions of 3-imino-(hydrazinylidene)-furan-2(3H)-ones derivatives with various nucleophilic reagents lead to the attack on the carbonyl group of the lactone fragment and to the for-mation of acyclic or heterocyclic structures [16][17][18][19][20][21] that retain the pharmacophore fragment of 2,4-dioxobutanoic acid [22][23][24][25][26][27][28][29][30][31][32]. This fragment was found in the structure of various biologically active and natural compounds [33,34], which indicates that this idea is worth developing.…”

Continuous‐Flow Synthesis of β‐Ketoesters and Successive Reactions in One‐Flow using Heterogeneous Catalysis

“…[8][9][10] β-Ketoesters are highly reactive intermediates in organic synthesis and they are widely used for the construction of heterocyclic structures [11,12] that make up bioactive molecules, [13] drug molecules, [14][15][16][17][18][19] and natural products. [20,21] Numerous synthetic strategies through CÀ C bond-formation processes have been explored, including Claisen condensation (Figure 1(a)) [22][23][24][25][26][27] and acylation; [28] however, the low pK a value of the proton at the α-position of β-ketoesters or high coordination abilities of their 1,3-dicarbonyl structures require the use of stoichiometric amounts of acids or strong bases in most cases.…”