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Heterocyclylalkylpiperidine derivatives, their preparation and compositions containing them

Heterocyclylalkylpiperidine derivatives of general formula (I) 1in their enantiomeric or diastereoisomeric forms or mixtures of these forms, and/or, where appropriate, in their syn or anti form or a mixture thereof, as well as any salt thereof.

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

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Influence of second coordination sphere hydroxyl groups on the reactivity of copper(I) complexes

We report the enhanced reactivity of hydroxyl substituted CuN 3+ derivatives, where N3 = tris(picolinyl) methane (tripic) and related derivatives, upon deprotonation of the O-H functionality. The work capitalizes on new methodology for incorporating hydroxyl groups into the second coordination sphere of copper centers. The key synthetic methodology relies on Pd-catalyzed coupling reactions of dilithiated 6-methyl-2-pyridone with bromopyridyl derivatives. These building blocks allow the preparation of tridentate N3 ligands with OH and OMe substituents flanking the fourth coordination site of a tetrahedral complex. Coupling of these tridendate ligands gives the corresponding hydroxy- and methoxy-functionalized bistripodal ligands. [Cu[bis(2-methylpyrid-6-yl)(2- hydroxypyrid-6-yl)methane](NCMe)]+ ([Cu(2H)(NCMe)]+) oxidizes readily in air to afford the mixed valence Cu1.5 dimer ([Cu2(2)2]+). Formation of [Cu 2(2)2]+ is accelerated in the presence of base and can be reversed with a combination of decamethylferrocene and acid. The reactivity of [Cu(2H)(NCMe)]+ with dioxygen requires deprotonation of the hydroxyl substituent: neither [Cu(tripic)(NCMe)]+ nor the methoxy-derivatives displayed comparable reactivity. A related mixed valence dimer formed upon oxidation of the dicopper(I) complex of a tetrahydroxy bis(tridentate) ligand, [Cu2(6H4)(NCMe)2] 2+. The dicopper(I) complex of the analogous tetramethoxy N 6-ligand, [Cu2(5)(NCMe)2]2+, instead reversibly binds O2. Deprotonation of [Cu(2H)(CO)]+ and [Cu(2H)(NCMe)]+ afforded the neutral derivatives Cu(2)(CO) and Cu2(2)2, respectively. The dicopper(I) derivative Cu 2(2)2 can be reoxidized, reprotonated, and carbonylated. The silver(I) complex, [Ag(2H)(NCMe)]BF4, forms an analogous neutral dimer (Ag2(2)2) upon deprotonation of the hydroxyl group. The structures of ligand 2H, [Cu2(5)(NCMe)2]+, [Cu2(2)2]+, [Cu2(6H 2)]+, [Ag(2H)(NCMe)]BF4, and Ag 2(2)2 were confirmed by single crystal X-ray diffraction.

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

New explortion of 1,1′-Bis(diphenylphosphino)ferrocene-palladium(II)dichloride dichloromethane complex

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Monodentate phosphine substitution in [Pd(kappa3-dppf)(PR3)][BF4]2 (dppf = 1,1?-bis(diphenylphosphino)ferrocene) compounds

The ligand 1,1?-bis(diphenylphosphino)ferrocene (dppf) is commonly employed in a variety of catalytic systems. There are a variety of coordination modes known for dppf, the least studied being the kappa3 coordination mode, in which both phosphorus atoms and the iron atom of dppf interact with another metal center. One such compound is the previously reported [Pd(kappa3-dppf)(PPh3)]2+. A series of related compounds, [Pd(kappa3-dppf)(P(p-C6H4R)3)]2+ (R = OCH3, CH3, F and CF3), has been synthesized and characterized. The X-ray crystal structure of [Pd(dppf)(P(p-C6H4F)3)][BF4]2 was determined. Electrochemical and computational studies indicate that the electron donor ability of the P(p-C6H4R)3 ligands influences the properties of these compounds. Substitution reactions of the P(p-C6H4R)3 ligands have been examined, and, in general, the more electron donating P(p-C6H4R)3 ligands completely replace the less electron donating ones. The kinetics of the reaction of [Pd(kappa3-dppf)(P(p-C6H4F)3)]2+ with P(p-C6H4OCH3)3 indicate that the reaction proceeds through a dissociative mechanism, contrary to the associative substitutions prevalent in square planar palladium(ii) 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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P2X7 MODULATORS

The present invention is directed to compounds of Formulas (I, IIa and IIb): The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, IIa and IIb). Methods of making and using the compounds of Formulas (I, IIa and IIb) are also within the scope of the invention.

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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 cross-coupling reaction of Grignard reagents with halobenzoic acids, halophenols and haloanilines

Convenient syntheses of substituted benzoic acids, phenols and anilines have been achieved by using palladium catalyzed cross-coupling reactions between Grignard reagents and aryl halides containing carboxy, hydroxy and amino groups without a protection-deprotection sequence.

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

Brief introduction of 1,1′-Bis(diphenylphosphino)ferrocene-palladium(II)dichloride dichloromethane complex

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Formula: C35H32Cl4FeP2Pd, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 95464-05-4, in my other articles.

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A METHOD OF INDOLE SYNTHESIS

The present invention relates to methods for the synthesis of indoles. In particular, the invention relates to the coupling of an a-haloenone or a-haloenal with an ortho-halonitroarene to form an ortho-(enone)nitroarene or ortho-(enal)nitroarene. Reductive cyclization of an ortho-(enone)nitroarene or ortho-(enal)nitroarene affords access to indole compounds.

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

Simple exploration of 1,1′-Bis(diphenylphosphino)ferrocene-palladium(II)dichloride dichloromethane complex

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MALEIC ACID DERIVATIVE, PRODUCTION METHOD FOR SAME, AND ANTI-CANCER COMPOSITION COMPRISING SAME

A maleic acid derivative represented by Chemical Formula 1 below or a pharmaceutically acceptable salt thereof: wherein, A is 5- to 7-membered phenyl having a substituent group, or heteroaryl or heterocycloalkyl containing at least one heteroatom selected from the group consisting of N, O, and S and having a substituent group, or 5- to 7-membered phenyl, heteroaryl, or heterocycloalkyl linked to C1-C5 straight- or branched-chain alkyl, wherein the substituent group is unsubstituted, halogen, OH, OR1, nitro, nitrile, NH2, NHR1, NR1R2 COOH, COOR1, CONH2, CONHR1, C1-C5 straight- or branched-chain alkyl, phenyl, heteroaryl, or 5- to 7-membered heterocycloalkyl, where R1 and R2 each are C1-C5 straight- or branched-chain alkyl, or phenyl or heteroaryl having a substituent group.

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

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PYRIDINE AND PYRIDIMINE COMPOUNDS AS PI3K-GAMMA INHIBITORS

The present disclosure provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that modulate the activity of phosphoinositide 3-kinases-gamma (PI3Kgamma) and are useful in the treatment of diseases related to the activity of PI3Kgamma including, for example, autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.

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

Extracurricular laboratory:new discovery of 1,1′-Bis(diphenylphosphino)ferrocene-palladium(II)dichloride dichloromethane complex

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A divergent synthesis of oligoarylalkanethiols with Lewis-basic N-donor termini

Araliphatic thiols are key molecules for the formation of self-assembled monolayers with high long-range order. If these monolayers shall act as bases for the attachment of other molecules, the respective thiols need to carry suitable functional groups, such as the amino or the pyridine group. Due to their Lewis-basicity, these groups are not compatible with the thiol group under most reaction conditions. Here, an entry into this versatile class of compounds is presented, by using fundamental building blocks in which the thiol groups are protected as triisopropylsilyl sulfides making them compatible with many reagents including Grignard reagents and palladium catalysts. With this strategy at hand, six thiols with bi- and terphenyl backbones, one to three methylene groups, and amino or pyridine head groups became accessible in short reaction sequences. 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

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Systematic studies on structural parameters for nanotubular assembly of hexa-peri-hexabenzocoronenes

Thirteen different hexa-peri-hexabenzocoronenes (HBCs) I-III were newly synthesized, and their self-assembling behaviors were investigated. Taking into account also the reported behaviors of amphiphilic HBCs, some structural parameters of HBC essential for the tubular assembly were revealed. Points to highlight include (1) the importance of two phenyl groups attached to one side of the HBC unit, (2) essential roles of long paraffinic side chains on the other side of the phenyl groups, and (3) no necessity of hydrophilic oligo(ethylene glycol) side chains. The hierarchical nanotubular structure, rendered by virtue of a synchrotron radiation technique, was virtually identical to our previous proposal, where the nanotubes are composed of helically coiled bilayer tapes with a tilting angle of ?45. Each tape consists of pi-stacked HBC units, where the inner and outer HBC layers are connected by interdigitation of paraffinic side chains. The coiled structure is most likely caused by a steric congestion of the phenyl groups attached to the HBC unit, whose tilting direction may determine the handedness of the helically chiral nanotube.

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