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The increasing number of people afflicted with diabetes throughout the world is a major health issue. Inhibitors of the sodiumdependent glucose cotransporters (SGLT) have appeared as viable therapeutics to control blood glucose levels in diabetic patents. Herein we report the discovery of LX2761, a locally acting SGLT1 inhibitor that is highly potent in vitro and delays intestinal glucose absorption in vivo to improve glycemic control.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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A full overview on the use of chiral phosphine-olefin ligands 1 in the rhodium-catalyzed asymmetric 1,4-addition of arylboronic acids to alpha,beta-unsaturated carbonyl compounds is described. Effective chiral environment of a Rh/1 complex was shown to resemble that of a Rh/(R,R)-Ph-bod* complex by comparing the experimental results as well as the X-ray crystal structures. High catalytic activity of a Rh/1 complex was disclosed and the catalytic cycle involving a trimer-monomer equilibrium was established through mechanistic studies using a reaction calorimeter and 31P NMR spectroscopy. A negative nonlinear effect derived from an inactive trimer-active monomer equilibrium of the catalyst was also successfully observed.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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Ongoing interest in the discovery of selective JAK3 inhibitors led us to design novel covalent inhibitors that engage the JAK3 residue Cys909 by cyanamide, a structurally and mechanistically differentiated electrophile from other cysteine reacting groups previously incorporated in JAK3 covalent inhibitors. Through crystallography, kinetic, and computational studies, interaction of cyanamide 12 with Cys909 was optimized leading to potent and selective JAK3 inhibitors as exemplified by 32. In relevant cell-based assays and in agreement with previous results from this group, 32 demonstrated that selective inhibition of JAK3 is sufficient to drive JAK1/JAK3-mediated cellular responses. The contribution from extrahepatic processes to the clearance of cyanamide-based covalent inhibitors was also characterized using metabolic and pharmacokinetic data for 12. This work also gave key insights into a productive approach to decrease glutathione/glutathione S-transferase-mediated clearance, a challenge typically encountered during the discovery of covalent kinase inhibitors.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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A convenient procedure for converting aryl alcohols to aryl fluorides via aryl nonafluorobutylsulfonates (ArONf) is presented. Moderate to good one-pot, two-step yields were achieved by this nonaflation and microwave-assisted, palladium-catalyzed fluorination sequence. The reductive elimination step was investigated by DFT calculations to compare fluorination with chlorination, proving a larger thermodynamic driving force for the aryl fluoride product. Finally, a key aryl fluoride intermediate for the synthesis of a potent HCV NS3 protease inhibitor was smoothly prepared with the novel protocol.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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Compounds having formula I, or pharmaceutically acceptable salts, hydrates or N-oxides thereof are provided and are useful for binding to CXCR7, and treating diseases that are dependent, at least in part, on CXCR7 activity. Accordingly, the present invention provides in further aspects, compositions containing one or more of the above-noted compounds in admixture with a pharmaceutically acceptable excipient.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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Optically pure hinckdentine A was synthesized on a 300 mg scale via an asymmetric catalysis-based strategy. The key steps to the first asymmetric synthesis involved (i) enantioselective dearomative cyclization of an achiral N-acyl indole that allowed for the efficient construction of the key polycyclic indoline intermediate with a crucial tetrasubstituted stereogenic carbon center, (ii) Beckmann fragmentation-mediated ring expansion, (iii) rearrangement-based introduction of an anilinic nitrogen atom, (iv) regioselective tribromination, and (v) final closure of the cyclic amidine moiety.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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A convergent approach to dibenzodioxocinones was explored, thereby racemic penicillide ((±)-1a) could be obtained in 13 steps in 4.2% overall yield, based on 5-amino-2-methylphenol (5) (Schemes 2-4).

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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Application of 53199-31-8, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.53199-31-8, Name is Bis(tri-tert-butylphosphine)palladium, molecular formula is C24H54P2Pd. In a article,once mentioned of 53199-31-8

The treatment of aryl iodides with tris(trimethylsilyl)silane in the presence of Pd(P(tBu)3)2 and the Huenig base leads to the formation of hypersilylated aromatic products in good to excellent yields without cleavage of weak Si-Si bonds under mild conditions. The Royal Society of Chemistry.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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Application of 32005-36-0, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, and a compound is mentioned, 32005-36-0, Bis(dibenzylideneacetone)palladium, introducing its new discovery.

Ylide-substituted phosphines (YPhos) have been shown to be excellent ligands for several transition metal catalyzed reactions. Investigations of the coordination behavior of the YPhos ligand YSPPh2 (1) [with YS = (Ph3P)(SO2Tol)C] toward group 9 and 10 metals revealed a surprisingly diverse coordination chemistry of the ligand. With Ni(CO)4, the formation of a di- as well as tricarbonyl complex is observed depending on the reaction conditions. In [(kappaP,I?2-benzene-1)Ni(CO)2] the phosphine ligand also coordinates via a phosphonium bound phenyl group to the metal leading to a unique nickel I?2-arene interaction, which can be viewed as an intermediate state toward P-C bond activation. Full cleavage of the P-C bond takes place with [Rh(COD)Cl]2 leading to a complex salt with [(kappaP,kappaO-1)Rh(COD)]+ as cation and a dirhodium trichloride complex anion. Here, YSPPh2 underwent P-C bond cleavage to thus act as an anionic diphosphine ligand. In contrast, in [(kappaP,kappaO-1)Rh(COD)]+ as well as [(kappaP,kappaO-1)Rh(CO)Cl], formed from the reaction of 1 with [Rh(CO)2Cl]2, the YPhos ligand acts as bidentate ligand complexing the metal via the phosphine and sulfonyl moiety with an intact PPh3 unit. A further type of coordination is observed with [Ir(COD)Cl]2. Here, phosphine coordination is accompanied by C-H activation at one of the phosphonium bound phenyl groups leading to a cyclometalated complex.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method

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Nano-Fe2O3-catalyzed borylation of arenes with diboron pinacol ester B2pin2 has been found to give borylation products with selectivity controlled by electronic effects of substituents. The Royal Society of Chemistry 2010.

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Reference:
Chapter 1 An introduction to palladium catalysis,
Palladium/carbon catalyst regeneration and mechanical application method