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We describe here the synthesis of dihydropyrimidines derivatives 3a-p, and evaluation of their alpha-glucosidase enzyme inhibition activities. Compounds 3b (IC50 = 62.4 ± 1.5 muM), 3c (IC50 = 25.3 ± 1.26 muM), 3d (IC50 = 12.4 ± 0.15 muM), 3e (IC50 = 22.9 ± 0.25 muM), 3g (IC50 = 23.8 ± 0.17 muM), 3h (IC50 = 163.3 ± 5.1 muM), 3i (IC50 = 30.6 ± 0.6 muM), 3m (IC50 = 26.4 ± 0.34 muM), and 3o (IC50 = 136.1 ± 6.63 muM) were found to be potent alpha-glucosidase inhibitors in comparison to the standard drug acarbose (IC50 = 840 ± 1.73 muM). The compounds were also evaluated for their in vitro cytotoxic activity against PC-3, HeLa, and MCF-3 cancer cell lines, and 3T3 mouse fibroblast cell line. All compounds were found to be non cytotoxic, except compounds 3f and 3m (IC50 = 17.79 ± 0.66-20.44 ± 0.30 muM), which showed a weak cytotoxic activity against the HeLa, and 3T3 cell lines. In molecular docking simulation study, all the compounds were docked into the active site of the predicted homology model of alpha-glucosidase enzyme. From the docking result, it was observed that most of the synthesized compounds showed interaction through carbonyl oxygen atom and polar phenyl ring with active site residues of the enzyme.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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The reaction of bis(dibenzylideneacetone)palladium(0) with white phosphorus was studied using the methods of NMR, UV spectroscopy, and X-ray powder diffraction. The products of the reaction are shown to be palladium phosphides, their composition depending on the ratio of the reagents. The mechanism of the formation of the palladium-enriched phosphides is suggested, which includes the formation of palladium diphosphide PdP2 that subsequently reacts with the excess of bis(dibenzylideneacetone)palladium(0) leading to palladium phosphides Pd5P2, Pd3P0.8, Pd 4.8P, and free dibenzylideneacetone. Pleiades Publishing, Ltd., 2012.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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The precursor nature effect on the state of the Pd?P surface layer in palladium catalysts and on their properties in the liquid-phase hydrogenation of chloronitrobenzenes under mild conditions has been investigated. A general feature of the Pd?P-containing nanoparticles obtained from different precursors and white phosphorus at P/Pd = 0.3 (PdCl2 precursor) and 0.7 (Pd(acac)2 precursor) is that their surface contains palladium in phosphide form (BE(Pd3d5/2) = 336.2 eV and BE(?2?) = 128.9 eV) and Pd(0) clusters (BE(Pd3d5/2) = 335.7 eV). Factors having an effect on the chemoselectivity of the palladium catalysts in chloronitrobenzenes hydrogenation are considered, including the formation of small palladium clusters responsible for hydrogenation under mild conditions.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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Two different enantioselective organocatalytic cascade reactions to form new sulfur-containing spirocyclic scaffolds are described. In the first approach, benzothiophen-2-one and enals react in the presence of a secondary amine catalyst through a Michael/Michael/Aldol sequence to afford the final spiro-cyclohexene carbaldehydes in good yields (up to 68 %) and with excellent selectivities [20:1 diastereomeric ratio (dr), up to 99 % ee]. In the second approach, the double Michael addition of benzothiophen-2-one to aromatic dienones with primary amine catalysis produces the corresponding spiro-cyclohexanones in good yields (up to 76 %) and with moderate-to-high selectivities (up to 12:1 dr, up to 90 % ee). Moreover, the use of N-phenylrhodanine as the bis-nucleophile for these reactions also allowed the formation of the corresponding spirocyclic adducts. Benzothiophenone and N-phenylrhodanine were successfully used as bis-nucleophiles in two enantioselective organocatalytic cascades. Their reactions with enals and dienones allowed the formation of new sulfur-containing spirocyclic scaffolds in good yields and with high selectivities. Copyright

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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The sulfur-carbon electrode, used as a cathode, appears to be an excellent source of nucleophiles which are good sulfuration reagents towards alkenes not substituted by leaving groups.However, the electrochemical reactions are often complex.It should be worth outlining that reaction leads to a vicarious substitution apparently specific of this kind of electrode.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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We herein report highly chemoselective transfer hydrogenation of alpha,beta-unsaturated carbonyl compounds to saturated carbonyls with formic acid as a hydrogen donor over a stable and recyclable heterogeneous Pd nanoparticles (NPs) on N,O-dual doped hierarchical porous biomass-derived carbon. The synergistic effect between Pd NPs and incorporated heteroatoms on carbon plays a critical role on promoting the reaction efficiency. A series of alpha,beta-aromatic and aliphatic unsaturated carbonyl compounds was selectively reduced to their corresponding saturated carbonyls in up to 97% isolated yields with good tolerance of various functional groups. In addition, the catalyst can be successively reused for at least 6 times without significant loss in reaction efficiency.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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A chemodivergent synthesis of two series of spirochromans depending on the catalytic system was developed. Starting from diarylideneacetones and organoboronic acids, asymmetric rhodium catalysis led to the enantioselective synthesis of 4,4?-disubstituted 2,2?-spirobichromans, while acid catalysis led to the formation of 4-substituted spirochroman-2,2?-chromenes. A plausible mechanism of the chemodivergent synthesis was proposed.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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Perfluoroalkylation of 2-vinylpyridine was conducted under conditions for the formation of low-valent nickel complexes during electroreduction of NiBr2L (L is the bipy, terpy) in DMF solutions. Depending on the electrosynthesis conditions, either dimeric products of addition of perfluoroalkyl substituents at the double bond of the olefin or (in the presence of triethylamine) 1-perfluorohexyl-2-pyridinethylene were formed.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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A novel direct transformation of hydrazones to acyloxylated pyrazoles by copper-catalyzed regioselective olefinic C(sp2)-H bond cycloamination and acyloxylation was performed under mild conditions, which combines the formation of the pyrazole skeleton and installation of an acyloxyl group in a single step, using facile carboxylic acids as the acyloxylation reagents.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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New strategies for the oxidative cycloaddition of enones with enamines are developed. These cycloaddition reactions directly afford substituted aromatic amines, which are important in organic chemistry, in moderate to good yield. Cu(OAc)2/TFA is shown to be essential to achieve high reaction efficiency.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate