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Provided is a fluoroboron compound which is highly safe and stable and is capable of forming a cyclic ether-fused ring by the intramolecular alkoxymethylation reaction, or a salt thereof. The compound can be synthesized by the intramolecular alkoxymethylation reaction of a fluoroboron compound represented by the formula (I) or a salt thereof in the presence of a metal catalyst. (wherein the moiety represented by the formula represents an aromatic ring; L represents a substituent such as a halogen atom; R represents a substituted or unsubstituted alkylene group having 1 or 2 carbon atoms; and M represents an alkali metal cation or the like, with the proviso that L and -R-OCH2BF3M are respectively located on contiguous carbon atoms on the aromatic ring, or in the case of a fused aromatic ring, on two carbon atoms adjacent to one carbon at the fused position).

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

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Palladium-catalyzed desulfitative Hiyama cross-coupling reactions of various arylsulfonyl chlorides with aryltriethoxysilane have been achieved in good yields. The reported cross-coupling reactions are tolerant to the common functional groups regardless of electron-withdrawing or electron-donating, making these transformations attractive alternatives to the traditional cross-coupling approaches.

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

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The invention relates to N-[(piperazinyl)hetaryl]arylsulfonamide compounds of the general formula I 1 in whichQ is a bivalent, 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Ra which is/are selected, independently of each other, from halogen, CN, NO2, CO2R4, COR5, C1-C4-alkyl and C1-C4-haloalkyl;Ar is phenyl or a 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Rb, which is/are selected from halogen, NO2, CN, CO2R4, COR5, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl and C1-C4-haloalkyl, with it also being possible for two radicals Rb which are bonded to adjacent C atoms of Ar to be together C3-C4-alkylene;R1 is hydrogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy-C1-C4-alkyl, C3-C4-alkenyl or C3-C4-alkynyl;with the radicals n, R1, R2, R3, R4 and R5 having the meanings given in the patent claims, to the N-oxides and to the physiologically tolerated acid addition salts of these compounds and to pharmaceutical compositions which comprise at least one N-[(piperazinyl)hetaryl]arylsulfonamide compound as claimed in one of claims 1 to 10 and/or at least one physiologically tolerated acid addition salt of I and/or an N-oxide of I, where appropraite together with physiologically accpetable carriers and/or auxiliary substances for treating diseases which respond to influencing by dopamine D3 receptor antagonists or agonists, in particular for treating diseases of the central nervous system and disturbances of kidney function.

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

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The invention relates to pyridinyl nicotinic acetylcholine receptor ligands, compositions comprising an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand and methods to treat or prevent a condition, such as depression and nicotine dependence, comprising administering to an animal in need thereof an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand

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

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Isoindigo-based conjugated polymers, PII2T-C6 and PII2T-C8, with carbosilane side chains have been designed and synthesized for stretchable electronic applications. The carbosilane side chains offerred a simple synthetic pathway to evaluate long and branched side chains in high yields and were prepared with a six or eight linear spacer plus two hexyl or octyl chains after branching. The studied polymers showed a high charge carrier mobility of 8.06 cm2 V-1 s-1 with an on/off current ratio of 106 as probed using a top-contact transistor device with organized solid state molecular packing structures, as investigated through grazing-incidance X-ray diffreaction (GIXD) and atomic force microscopy (AFM) technique systematically. The studied polymers, more attractive, exhibited superior thin film ductility with a low tensile modulus in a range of 0.27-0.43 GPa owing to the branched carbosilane side chain, and their mobility was remained higher than 1 cm2 V-1 s-1 even under a 60% strain along parallel or perpendicular direction to the tensile strain. Such polymer films, in addition, can be simultaneously operated over 400 stretching/releasing cycles and maintained stable electrical properties, suggesting the newly designed materials possessed great potential for next-generation skin-inspired wearable electronic application with high charge carrier mobility, low tensile modulus, and stable device characteristics during stretching.

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

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An expeditious approach to catalytic enantioselective total syntheses of crinine-type Amaryllidaceae alkaloids has been accomplished via a Pd-catalyzed enantioselective decarboxylative allylation of allylenol carbonates as a key step (up to 96% ee). Using this strategy, collective total syntheses of Amaryllidaceae alkaloids such as (-)-epi-elwesine (1b), (-)-crinine (1c), (-)-epi-crinine (1e), (-)-oxocrinine (1f), and (-)-buphanisine (1d) have been accomplished. Gratifyingly, naturally occurring Amaryllidaceae alkaloids such as (+)-vittatine (1g), (+)-epi-vittatine (1h), and (+)-epi-elwesine (1i) [enantiomers of (-)-1c, (-)-1e, and (-)-1b, respectively] have also been achieved by switching the antipode of ligand used in the catalytic enantioselective step.

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

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Identifying the biological origin of a disease and the potential targets for intervention are some of the first steps in the discovery of a medicine. The metabotropic glutamate receptor 4 (mGlu4) has lately received much attention due to its potential role in various neuronal diseases such as Parkinson’s disease (PD) and other disorders. To better understand the role of mGlu4 in health and disease conditions, we were interested in developing an mGlu4-selective radiotracer for in vivo studies. Herein we discuss our efforts to develop novel mGlu4 positron emission tomography (PET) radiotracers from mGlu4 positive allosteric modulators (PAMs). We have investigated the biology of this receptor in vitro using cells expressing mGlu4, as well as in vivo, using the 6-hydroxydopamine (6-OHDA)-lesion rat model of Parkinson’s disease. Results of cell studies showed the important role of endogenous glutamate in inducing changes in the affinity of allosteric modulators of mGlus. Results from PET imaging studies showed the interplay between presynaptic mGlu4 and postsynaptic mGlu5 expression in the lesioned side of the brain, while the results of pharmacological MRI studies of the hemodynamic response showed enhanced signal changes in cortical areas in the lesioned side after challenge with mGlu4 PAMs or mGlu5 negative allosteric monitors (NAMs).

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

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Palladium allyl, cinnamyl, and indenyl complexes with the ylide-substituted phosphines Cy3P+?C?(R)PCy2 (with R=Me (L1) or Ph (L2)) and Cy3P+?C?(Me)PtBu2 (L3) were prepared and applied as defined precatalysts in C?N coupling reactions. The complexes are highly active in the amination of 4-chlorotoluene with a series of different amines. Higher yields were observed with the precatalysts in comparison to the in situ generated catalysts. Changes in the ligand structures allowed for improved selectivities by shutting down beta-hydride elimination or diarylation reactions. Particularly, the complexes based on L2 (joYPhos) revealed to be universal precatalysts for various amines and aryl halides. Full conversions to the desired products are reached mostly within 1 h reaction time at room temperature, thus making L2 to one of the most efficient ligands in C?N coupling reactions. The applicability of the catalysts was demonstrated for aryl chlorides, bromides and iodides together with primary and secondary aryl and alkyl amines, including gram-scale applications also with low catalyst loadings of down to 0.05 mol %. Kinetic studies further demonstrated the outstanding activity of the precatalysts with TOF over 10.000 h?1.

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

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Subtle modulation of the electronic properties of the dibenzylideneacetone (dba) ligand allows the development of an efficient protocol for the Heck alkenylation of 5-iodo-2?-deoxyuridine. This protocol enables the large-scale synthesis of commercially important nucleoside building blocks. The isolation of one key molecule was accomplished under column-free conditions on a 10-gram scale.

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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 general and highly enantioselective arylation of carbamates derived from primary alcohols was developed by combining Hoppe’s sparteine-mediated asymmetric lithiation with Negishi cross-coupling. Coupled with Aggarwal’s lithiation-borylation sequence, the current method provides a short and divergent access to a variety of enantioenriched secondary and tertiary benzylic alcohols.

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