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The catalytic efficiency of a bifunctional chiral thiourea derived from L-proline was evaluated in the asymmetric direct vinylogous Michael reaction of α,α-dicyanoolefins to β-nitrostyrenes with an electron- releasing or electron-withdrawing substituent in various positions. The corresponding adducts were isolated in good yields, with excellent diastereo- (>99%) and enantioselectivity (up to 95%). The Michael adducts were further functionalized to achieve the synthesis of polycyclic fused pyrrolidines with three contiguous stereocenters in good enantioselectivities. [ABSTRACT FROM AUTHOR]

A new synthetic strategy to construct spirooxindole-naphthopyran scaffold has been demonstrated via Friedel-Crafts type/hemiketalization of oxindole α-ketoester with 2-naphthol. Under the established reaction condition, quaternary chiral center at C3-position of oxindole has been created with very good asymmetric induction up to 98 % for a broad range of substrates. DFT calculations, which account for the stereochemical outcome, were performed. [ABSTRACT FROM AUTHOR]

Copper(I) bromide catalyzed direct C-H arylation of cyclic enamides was achieved using diaryliodonium salts in the absence of base/additive at ambient temperature with high yields. A biologically active dihydro[a]benzocarbazole scaffold was synthesized using the established protocol. The scope of the current methodology was further extended for the synthesis of C4-, C7-aryl-substituted 1-naphthyl acetamides in good yields. [ABSTRACT FROM AUTHOR]

Chiral Lewis bases facilitated the synthesis of highly functionalized spirooxindoles containing α- exo-methylene-γ-butyrolactones in high yields (76-92 %) and excellent enantioselectivities (up to 98 % ee) at ambient temperature. [ABSTRACT FROM AUTHOR]

Tartrate-derived bioxazoline ligands, which form a five-membered chelate ring with metals, were evaluated for use in the asymmetric allylic alkylation (AAA) reactions of various symmetrical and unsymmetrical allyl acetates. Excellent enantioselectivities were achieved by using both symmetrical and unsymmetrical allyl acetates. [ABSTRACT FROM AUTHOR]

Derivatives of 2,3-dihydroquinazolinones (2,3-DHQZs) are prized for their prevalent pharmaceutical applications. Although there are potential applications, methods available for the enantioselective synthesis of these valuable compounds are scarce, since the chiral aminal center is prone to racemization. We have overcome the difficulties in the catalytic enantioselective synthesis of 2,3- DHQZs using Sc(III)-inda-pybox as a catalyst, in a process with a broad substrate scope [ABSTRACT FROM AUTHOR]

Enantioselective synthesis of 2,3-dihydroquinazolinones (DHQZs) was accomplished using readily available Sc(III)-inda-pybox as the catalyst. This is the first report on the metal catalyzed asymmetric intramolecular amidation of imines to synthesize DHQZs. [ABSTRACT FROM AUTHOR]

starting from various oxindole α-ketoester and 2-naphthol [ABSTRACT FROM AUTHOR]

An abstract of the article "Assembly of 3-Allyl-3-ethynyl-oxindole Motifs via Palladium(II)-Catalyzed Quaternary Allylation of 3-Ethynyl-3-OBoc-oxindoles" by N. Kumarswamyreddy and colleagues is presented.

A direct, high-yielding C-H arylation at position 2 of cyclic enamides of type (I) becomes possible in the presence of CuBr as the catalyst at room temperature. [ABSTRACT FROM AUTHOR]

The bisoxazoline (BOX) is found to be an efficient ligand in Pd-catalyzed asymmetric allylic alkylation. [ABSTRACT FROM AUTHOR]

A chart is presented related to chemical reaction of fused pyrimidine derivatives which depicts enantioselective synthesis of 2,3-dihydroquinazolinones using Sc(III)-inda-pybox.

A Sc-catalyzed tandem imination/intramolecular amidation of anthranilamide with different aldehydes can be achieved with good to excellent enantioselectivity in the presence of an inda-pybox catalyst. [ABSTRACT FROM AUTHOR]

Fat mass obesity-associated protein (FTO) is a DNA/RNA demethylase involved in the epigenetic regulation of various genes and is considered a therapeutic target for obesity, cancer, and neurological disorders. Here, we aimed to design novel FTO-selective inhibitors by merging fragments of previously reported FTO inhibitors. Among the synthesized analogues, compound 11b , which merges key fragments of Hz ( 3 ) and MA ( 4 ), inhibited FTO selectively over alkylation repair homologue 5 (ALKBH5), another DNA/RNA demethylase. Treatment of acute monocytic leukemia NOMO-1 cells with a prodrug of 11b decreased the viability of acute monocytic leukemia cells, increased the level of the FTO substrate N 6 -methyladenosine in mRNA, and induced upregulation of MYC and downregulation of RARA , which are FTO target genes. Thus, Hz ( 3 )/MA ( 4 ) hybrid analogues represent an entry into a new class of FTO-selective inhibitors.