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2-(1,2,3-TRIAZOL-2-YL)BENZAMIDE AND 3-(1,2,3-TRIAZOL-2-YL)PICOLINAMIDE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS

The present invention relates to 2-(1,2,3-triazol-2-yl)benzamide and 3-(1,2,3-triazol-2-yl)picolinamide derivatives of formula (I) wherein Ar1, Q, and R1 to R5 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.

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

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A 3 – halogenated -4 – alkoxy quinoline compound and its preparation method and application (by machine translation)

The invention discloses a 3 – halo – 4 – alkoxy quinoline compound and its preparation method and application, the 3 – halo – 4 – alkoxy quinoline compounds of the formula (II) structural formula as shown: ; Wherein Ar is aromatic group; R is an aromatic group, substituted aromatic group, alkyl, substituted alkyl or heterocyclic group; R ‘ is alkyl, substituted alkyl, aromatic group or substituted aromatic group; X is a halogen atom. The present invention provides a 3 – halo – 4 – alkoxy in the quinoline compound containing 4 – alkoxy quinoline pharmocology, has very good biological activity, such as anti-HIV, malaria and anti-fungi, can be used as the chemical or pharmaceutical intermediates. The 3 – halo – 4 – alkoxy quinoline compound it is potent anti-cancer medicines and anti-cancer drug of the key frame structure, in the preparation of anticancer drugs in the field has a very broad application prospect. (by machine translation)

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

Final Thoughts on Chemistry for 52409-22-0

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An aryl carboxylic acid ester compound for catalytic synthesis of (by machine translation)

The invention provides a method for catalysis synthesizing of an aryl formic ether compound represented by the formula (III) shown in the description. The method comprises the step of reacting a compound represented by the formula (I) shown in the description and a compound represented by the formula (II) shown in the description in an organic solvent in the presence of a palladium compound-phosphonic compound composite catalyst, an accelerator and alkali so as to obtain the compound represented by the formula (III) shown in the description, wherein R is H, C1-C6 alkyl or halogen; and X is halogen. By means of selection and synergistic effects of the composite catalyst, the accelerator and the alkali, a target product is obtained with high yield; and the method can be widely applied in the technical field of organic synthesis, such as medical intermediate synthesis, and has good industrial application potential and prospect.

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

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Palladium catalyzed direct C-2 arylation of indoles

The synthesis and catalytic evaluation of palladium complexes containing NCN Pincer ligand is reported. The pincer palladium complexes as (pre)catalyst showed efficient catalytic activity for the C-H arylation of N-substituted indoles, allowing the synthesis of 2-arylindoles with moderate to good yields and excellent regioselectivities.

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

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3-Aryl-3-(isoxazol-3-yl)propanoic Acids and 2-Aryloxyacetic Acids as Potent GPR40 Agonists

GPR40 is one of the most prominent targets for the treatment of type 2 diabetes (T2DM), and has its role in insulin secretion via blood-glucose-dependent manner with a minimum risk of hypoglycemia. In order to discover novel antidiabetics bearing these benefits, we screened various derivatives with two distinct pharmacophores. Both series displayed potent agonistic activities for GPR40 in vitro functional assay. Through additional ADME and in vivo efficacy evaluations, we identified the potent hit candidate 2j as a novel GPR40 agonist.

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

The important role of Pd2(DBA)3

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Synthesis and characterization of substituted poly(naphthalene)s with imine bonding containing thiophene unit

In this study, 5-(4H-dithieno[3,2-b:2?,3?-d]pyrrol-4-yl)naphthalen-1-amine was synthesized from the required reaction conditions of 3,3?-dibromo-2,2?-bithiophene with 1,5-diamine naphthalene. Then, Schiff base monomers were synthesized from the condensation reactions of 5-(4H-dithieno[3,2-b:2?,3?-d]pyrrol-4-yl)naphthalen-1-amine with mono aldehydes such as 2-hydroxybenzaldehyde, 4-hydroxybenzaldehyde and isovaniline. The Schiff base monomers were polymerized via oxidative polycondensation in 0.1 M KOH aqueous solution at 90 C by 10?15% NaOCl oxidant. The structures of synthesized compounds were carried out by FT-IR, UV?Vis, 1H NMR, 13C NMR techniques. Further characterization was implemented by cyclic voltammetry (CV) electrochemical properties, fluorescence (FL) measurements, electrical properties, thermogravimetric-differential thermal analysis (TG-DTA) and differential scanning calorimetry (DSC) measurements. Depending on structural changes of synthesized polymers, differences were observed for the optical, electrochemical, thermal and physical properties. The optical and electrochemical band gaps, conductivity and fluorescence properties of P1 were found to be better than other polymers. The fluorescence intensity of P1 in two different wavelengths was found to be 632 a.u. and 1000 a.u. The optical (Eg) and electrochemical band gap values (E’g) of P1 were found to be 2.34 and 2.25 eV, respectively. This low band gap values have demonstrated to be a good conjugation in the structure. According to TG measurements, Ton temperature of P1, P2 and P3 were found to be 227, 293 and 306 C, respectively. The weight average molecular weight (Mw) of P1, P2 and P3 were calculated to be 39500, 40150 and 44300 Da, respectively.

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

The important role of Pd2(DBA)3

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Synthesis of 2,2-diaryl-1,1-difluoroethenes via Pd-catalyzed dehydrosulfonylative cross-coupling of alpha-[difluoro(phenylsulfonyl)methyl]benzyl tosylates with arylboronic acids

By using PhSO2CF2H as the difluoromethylidene equivalent, a novel method for connecting aromatic aldehydes and arylboronic acids via consecutive reactions was developed to obtain structurally diverse 2,2-diaryl-1,1-difluoroethenes. The key step is the palladium-catalyzed dehydrosulfonylative cross-coupling of tosylates that are prepared from PhSO2CF2H, aromatic aldehydes and tosyl chloride. Mechanistic investigations showed that the reaction proceeds mainly through base-mediated dehydrosulfonylation followed by palladium-catalyzed C(sp2)-C(sp2) cross-coupling reaction.

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

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Synopsis of recent synthetic methods and biological applications of phosphinic acid derivatives

The chemistry of phosphinic acid derivatives has attracted increasing attention in both synthetic organic and biological fields, and great progress in the application of such compounds has been achieved in recent years. This review aims to document a systematic account of the prevailing methods for the synthesis of acyclic/cyclic phosphinic acids either in enantiopure or in racemic form. The most important among them are Hirao cross-coupling reaction, Michael addition to olefins, Atherton?Todd reaction and Michaelis-Arbuzov reaction. Other noteworthy methods applied for this purpose are benzylation and allylation of hypophosphorous acid, hydrophosphinylation of aldehydes or alkenes and phosphorylation of strained P-heterocycles. Parallel synthetic methods leading to heterocyclic phosphinic acids such as phospholes, azaphospholidines, phosphorines, 1,2-oxaphosphorines, 1,3-azaphosphorines, 1,4,2-oxazaphosphinanes, phosphindoles, and benzazaphosphorines are also disclosed. Finally, selected significant applications in medicinal chemistry of the title compounds like Zn-metalloprotease Inhibitors, prodrug and drug applications are described briefly here. The bibliography includes 304 references.

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

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Direct introduction of a naphthalene-1,8-diamino boryl [B(dan)] group by a Pd-catalysed selective boryl transfer reaction

A non-symmetrical diboron reagent, B(pin)-B(dan), has been utilised in the Pd-catalysed borylation of aryl bromides and chlorides. Remarkably selective formation of aryl-B(dan) bonds is established. This represents a direct and efficient way to introduce masked boronic acids. The synthetic usefulness of this reaction is demonstrated in the preparation of boron-differentiated di- and polyboron compounds.

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

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Thermoresponsive core-shell nanoparticles with cross-linked pi-conjugate core based on amphiphilic block copolymers by RAFT polymerization and palladium-catalyzed coupling reactions

Well-defined amphiphilic block copolymers composed of S-vinyl sulfides and N-isopropyl acrylamide (NIPAM) were synthesized by reversible addition-fragmentation chain transfer (RAFT) polymerization. Thermoresponsive core-shell nanoparticles with cross-linked pi-conjugate cores were obtained by in situ cross-linking reactions between 4-bromophenyl moieties in the block copolymers and diboronic acids or a diamine compound in the presence of a palladium catalyst following micelle formation in ethanol/H2O or ethanol. We initially investigated RAFT polymerization of two S-vinyl sulfide derivatives, namely phenyl vinyl sulfide (PVS) and 4-bromophenyl vinyl sulfide (BPVS), using a dithiocarbamate-type chain transfer agent (CTA). Then, RAFT polymerization of NIPAM using poly(S-vinyl sulfide) macro-CTAs was conducted to synthesize the amphiphilic block copolymers. Suzuki and Buchwald-Hartwig coupling reactions were found to be effective in the preparation of core-shell nanoparticles with thermoresponsive shells and cross-linked optoelectronic cores. The resulting nanoparticles showed characteristic thermoresponsive properties, as confirmed by turbidity and dynamic light scattering measurements. Stable and uniform core cross-linked nanoparticles were successfully prepared by the in situ palladium-catalyzed coupling reactions, and the optoelectronic and thermoresponsive properties of the nanoparticles could be tuned depending on the nature of the difunctional coupling agents, reaction conditions, and comonomer composition of the block copolymers.

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