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Thiocarbonyl Surrogate via Combination of Sulfur and Chloroform for Thiocarbamide and Oxazolidinethione Construction

An efficient and practical thiocarbonyl surrogate via combination of sulfur and chloroform has been developed. A variety of thiocarbamides and oxazolidinethiones have been established, including chiral thiourea catalysts and chiral oxazolidinethione auxiliaries with high selectivity. Meanwhile, pesticides Diafenthiuron (an acaricide), ANTU (a rodenticide), and Chloromethiuron (an insecticide) were practically synthesized through this method in gram scale. Dicholorocarbene, as the key intermediate, was further confirmed via a carbene-trapping control experiment.

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

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BENZOLACTAM COMPOUNDS AS PROTEIN KINASE INHIBITORS

The invention provides a compound of formula (0): or a pharmaceutically acceptable salt, N-oxide or tautomer thereof. The compounds are inhibitors of ERK 1/2 kinases and will be useful in the treatment of ERKl/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

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Synthesis and Application of Branched Type II Arabinogalactans

The synthesis of linear and (1 ? 6)-branched beta-(1 ? 3)-d-galactans, structures found in plant arabinogalactan proteins (AGPs), is described. The synthetic strategy relies on iterative couplings of monosaccharide and disaccharide thioglycoside donors, followed by a late-stage glycosylation of heptagalactan backbone acceptors to introduce branching. A key finding from the synthetic study was the need to match protective groups in order to tune reactivity and ensure selectivity during the assembly. Carbohydrate microarrays were generated to enable the detailed epitope mapping of two monoclonal antibodies known to recognize AGPs: JIM16 and JIM133.

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

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COMPOUNDS FOR USE IN IMAGING, DIAGNOSING AND/OR TREATMENT OF DISEASES OF THE CENTRAL NERVOUS SYSTEM

This invention relates to novel compounds suitable for labelling by 18F and the corresponding 18F labelled compounds themselves, 19F-fluorinated analogues thereof and their use as reference standards, methods of preparing such compounds, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by Positron Emission Tomography (PET).

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

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Copper Bis(oxazoline)-Catalyzed Enantioselective Alkynylation of Benzopyrylium Ions

The stereocontrolled construction of biologically relevant chromanones and tetrahydroxanthones has been achieved through the addition of alkynes to benzopyrylium trilfates under the influence of copper bis(oxazoline) catalysis. Excellent levels of enantiocontrol (63?98 % ee) are achieved in the addition of a variety of alkynes to an array of chromenones with a hydrogen in the 2-position. Promising levels of enantiocontrol (54?67 % ee) are achieved in the alkynylation of chromenones with esters in the 2-position, generating tertiary ether stereocenters resembling those frequently found in naturally occurring metabolites.

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

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Reaction of a zirconocene-carboryne complex with pyridines: Ligand C-H activation

Reactions ofCp2Zr(mu-Cl)(mu-C2B10H 10)Li(OEt2)2 (1) with various N-heterocycles derived from pyridine were studied. Treatment of 1 with pyridine, 2-bromopyridine, 2, 4-lutidine, quinoline, and 2-(1-hexynyl)pyridine generated alpha-C-H activation (sigma-bond metathesis) products Cp2Zr(eta2-C, N-C5H4N)(sigma-C2B10H11) (2), Cp2Zr[eta2-C,N-(6-Br-C5H 3NN)](sigma- C2B10H11) (3), Cp2Zr[eta2-C,N-(4,6-Me2-C5H2N)] (sigma-C2B10H11) (4), Cp2Zr(eta2-C,N-C9H6N)(sigma-C2B10H11) (5), and Cp2Zr- {eta2-C,N-[6-(nBuCtC)-C5H3NN]}(sigma-C2B10H11) (7), respectively. On the other hand, reaction of 1 with acridine gave the addition product 1,2-[Cp2Zr(10,9-C13H9N)]-1,2-C2B10H 10 (6) in 85% isolated yield. Complex 1 reacted with 3-(1-hexynyl)pyridine to afford alpha-C-H activation species Cp2Zr{eta2-C,N-[5-(nBuCtC)C5H3NN]}(sigma-C2B10H11) (8a) andCp2Zr{eta2-C,N-[3-(nBuCtC)C5H3NN]}-(sigma- C2B10H11) (8b) in a molar ratio of 42:58, as determined by the 1H NMR spectrum. In the presence of CuI, however, the CtC insertion products zirconacyclopentenes 1,2-[Cp2ZrC(2-C5H4N)dCR]-1,2-C2B10H10 [R = Bun (9), Ph (10)] were obtained in 74-77% yields. It is suggested that the coordination of pyridine to the Zr atom is crucial for alpha-C-H activation (sigma-bond metathesis). The presence of CuI can alter the reaction path by preventing the coordination of pyridine to the Zr atom, which blocks the alpha-C-H activation path, leading to the alkyne insertion reaction. All complexes were characterized by 1H, 13C, and 11B NMR spectra as well as elemental analyses. Their structures were further confirmed by single-crystal X-ray analyses.

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

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Heterogeneous catalytic oxidation of pyridines to N-oxides under mild conditions using tungsten-loaded TiO2

The heterogeneous catalytic oxidation of pyridines to pyridine N-oxides has been studied using tungsten-loaded TiO2as the catalyst and hydrogen peroxide as the green oxidant. The catalysts were synthesized by a simple impregnation technique and characterized by X-ray powder diffraction, Raman spectroscopy, transmission electron microscopy, energy dispersion X-ray spectroscopy, X-ray photoelectron spectroscopy. The catalytic performances of the catalysts were evaluated by the N-oxidation of pyridines with 30?wt% H2O2solution as an environmentally friendly oxidant at room temperature. These processes serve as an efficient method to prepare a variety of pyridine-N-oxides in modest to high yields, and the pyridine N-oxides could be easily separated from the heterogeneous catalytic system. This study will provide a useful strategy for preparation of heterocyclic N-oxides in the mild condition.

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

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Synthesis of enantiomerically pure cis- and trans-1,2- diaminoindanes

The four isomers of cis- and trans-1,2-diaminoindanes 5 and 11 were prepared in three steps and high enantiomeric excess by a key lipase- catalyzed selective transesterification of racemic cis-2-azido-1-indanol and trans-1-azido-2-indanol, respectively.

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

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Preparation of N-chlorothio(methyl)carbamoyl halides

A process for the preparation of N-chlorothio(methyl)carbamoyl halides.

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

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Microwave promoted synthesis of cycl[3.2.2]azines in water via a new three-component reaction

A microwave-promoted and base-catalyzed synthesis of cycl[3.2.2]azines is accomplished in water via a three-component reaction (3-CR) of 2-picoline, alpha-bromoacetophenone and alkyne. The extension of the methodology to the synthesis of steroidal and carbocyclic cycl[3.2.2]azine is also reported.

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Reference£º
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis