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There are provided N-aralkyl piperidine derivatives which are selective sigma receptor antagonists. These compounds and pharmaceutical compositions containing them are useful for treating physiological or drug induced psychosis or dyskinesia in a mammal.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H15210N – PubChem

 

26/9/2021 News A new application about 67686-01-5

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An in-water dehydrative alkylation with a novel heterobimetallic polymeric catalyst is described. Thus, a boron-iridium heterobimetallic polymeric catalyst was prepared by ionic convolution of a poly(catechol borate) and an iridium complex. The alkylation of ammonia and amines with alcohols, alkylating agents, was performed with 1 mol % Ir of the heterogeneous catalyst in water without the use of organic solvents under aerobic conditions to give the corresponding alkylated amines.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H15252N – PubChem

 

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Novel unsaturated ether derivatives of alkyl piperidine and pyrrolidine compounds, pharmaceutical compositions containing them, methods of preparation and methods of using these compounds as antipsychotic agents are disclosed.

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Piperidine – Wikipedia,
Piperidine | C5H15237N – PubChem

 

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Regioisomers of 3,5-diphenyl-1-(4-(trifluoromethyl)phenyl)-1H-pyrazole-based palladacycles (1 and 2) were synthesized by the aromatic C-H bond activation of N/3-aryl ring. The application of these regioisomers as catalysts to enable the formation of alpha-alkylated ketones or quinolines with alcohols using a hydrogen borrowing process is evaluated. Experimental results reveal that palladacycle 2 is superior over palladacycle 1 to catalyze the reaction under similar reaction conditions. The reaction mechanisms for the palladacycles 1 and 2 catalyzed alpha-alkylation of acetophenone were studied using density functional theoretical (DFT) methods. The DFT studies indicate that palladacycle 2 has an energy barrier lower than that of palladacycle 1 for the alkylation reaction, consistent with the better catalytic activity of palladacycle 2 seen in the experiments. The palladacycle-phosphine system was found to tolerate a wide range of functional groups and serves as an efficient protocol for the synthesis of alpha-alkylated products under solvent-free conditions. In addition, the synthetic protocol was successfully applied to prepare donepezil, a drug for Alzheimer’s disease, from simple starting materials.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H15232N – PubChem

 

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The iron storage protein bacterioferritin (BfrB) is central to bacterial iron homeostasis. The mobilization of iron from BfrB, which requires binding by a cognate ferredoxin (Bfd), is essential to the regulation of cytosolic iron levels in P. aeruginosa. This paper describes the structure-guided development of small molecule inhibitors of the BfrB-Bfd protein-protein interaction. The process was initiated by screening a fragment library and followed by obtaining the structure of a fragment hit bound to BfrB. The structural insights were used to develop a series of 4-(benzylamino)- A nd 4-((3-phenylpropyl)amino)-isoindoline-1,3-dione analogs that selectively bind BfrB at the Bfd binding site. Challenging P. aeruginosa cells with the 4-substituted isoindoline analogs revealed a dose-dependent growth phenotype. Further investigation determined that the analogs elicit a pyoverdin hyperproduction phenotype that is consistent with blockade of the BfrB-Bfd interaction and ensuing irreversible accumulation of iron in BfrB, with concomitant depletion of iron in the cytosol. The irreversible accumulation of iron in BfrB prompted by the 4-substituted isoindoline analogs was confirmed by visualization of BfrB-iron in P. aeruginosa cell lysates separated on native PAGE gels and stained for iron with Ferene S. Challenging P. aeruginosa cultures with a combination of commercial fluoroquinolone and our isoindoline analogs results in significantly lower cell survival relative to treatment with either antibiotic or analog alone. Collectively, these findings furnish proof of concept for the usefulness of small molecule probes designed to dysregulate bacterial iron homeostasis by targeting a protein-protein interaction pivotal for iron storage in the bacterial cell.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H15221N – PubChem

 

Extracurricular laboratory:new discovery of (1-Benzylpiperidin-4-yl)methanol

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5, 6 – dimethoxy – 1 – oxo – 2, 3 – dihydro – 1H – indene – 2 – to (a) the present invention refers to a group represented by the formula 3 formula 4 […][…] represented benzylpiperidine compound reacting to the presence of a base, to 2 – oxo – 5, 6 – dimethoxy – 1 – ((1 – benzylpiperidine – 4 – yl) methyl) represented by the formula 2 – 2, 3 – dihydro – 1H – indene – 2 – […][…] step number tank; and (b) 2 – oxo – 5, 6 – dimethoxy – 1 – ((1 – benzylpiperidine – 4 – yl) methyl) of said formula 2 formula 1 – 2, 3 – dihydro – 1H – indene – 2 – de […][…] hydrocyanation reaction (decyanation reaction) of a method including the step number it goes roundlung questionlung qualityit goes round caused by representative number bath tank number under public affairs substrate. (by machine translation)

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H15266N – PubChem

 

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A method for synthesizing N – ethyl carbazole, relates to N – ethyl carbazole. In N – methyl pyrrolidine in, the carbazole with proton removing agent for salt forming reaction, generating carbazole salt, to continue to access the acetylene after reaction, to obtain N – vinyl carbazole; generates a N – vinyl carbazole in organic solvent, then adding Pd catalyst, the hydrogenation reaction in the auxiliary agent, to obtain N – ethyl carbazole. Preferably a series of special catalyst, by catalytic hydrogenation process can be realized effectively N – ethyl carbazole green synthesis, reduce the three waste discharge. In the hydrogenation process, catalyst can be reused, the cost is reduced. The hydrogenation process of the prepared N – ethyl carbazole and higher product quality. Do not require traditional alkylation reagent (sulfur acid ethyl ester, ethyl carbonate, such as halogen ethane) and the toxic organic solvent to participate in, the problem of the discharge without waste, is a truly accord with the green clean production process. (by machine translation)

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H15260N – PubChem

 

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Based on the definition of a 5-HT4 receptor antagonist pharmacophore, a series of pyrrolo[1,2-a]thieno[3,2-e] and pyrrolo[1,2-a]thieno[2,3-e] pyrazine derivatives were designed, prepared, and evaluated to determine the properties necessary for high-affinity binding to 5-HT4 receptors. The compounds were synthesized by substituting the chlorine atom of the pyrazine ring with various N-alkyl-4-piperidinylmethanolates. They were evaluated in binding assays with [3H]GR113808 (1) as the 5-HT4 receptor radioligand. The affinity values (Ki or inhibition percentages) were affected by both the substituent on the aromatic ring and the substituent on the lateral piperidine chain. A methyl group on the tricyclic ring produced a marked increase in affinity while an N-propyl or N-butyl group gave compounds with nanomolar affinities. Among the most potent ligands, 34d was selected for further pharmacological studies and evaluated in vivo. This compound acts as an antagonist/weak partial agonist in COS-7 cells stably expressing the 5-HT4(a) receptor and is of great interest as a peripheral antinociceptive agent.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H15249N – PubChem

 

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Polymeric bimetallic catalyst-promoted in-water dehydrative alkylation of ammonia and amines with alcohols

A dehydrative alkylation with three kinds of Ir/B heterobimetallic polymeric catalysts in water is reported. The polymeric heterobimetallic catalysts were readily prepared by ionic convolution of a poly(catechol borate) and iridium complexes. The N-alkylation of ammonia and amines with alcohols, as alkylating agents, was carried out with a heterogeneous catalyst (1 mol% Ir) at 100 C without the use of organic solvents under aerobic and aqueous conditions to afford the corresponding alkylated amines in high yield. Georg Thieme Verlag Stuttgart New York.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H15262N – PubChem

 

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Structure-activity relationship studies of novel 4-[2-[bis(4- fluorophenyl)methoxy]ethyl]-1-(3-phenylpropyl)piperidine analogs: Synthesis and biological evaluation at the dopamine and serotonin transporter sites

Several analogs of the potent dopamine (DA) transporter ligand 4-[2- [bis(4-fluorophenyl)-methoxy]ethyl]-1-(3-phenylpropyl)piperidine, 1b, were made and biologically evaluated for their binding at the DA and serotonin (5HT) transporters in rat striatal membranes. Different alkyl chain lengths and substitutions were introduced in these molecules to generate an optimum activity and selectivity for the DA transporter. In general, unsubstituted and fluoro-substituted compounds were the most active and selective for the DA transporter. The compound 4-[2(diphenylmethoxy)ethyl]-1-benzylpiperidine, 9a, showed high potency and was the most selective for the DA transporter (5HT/DA = 49) in this series of compounds. Some of these novel analogs were found to be more selective in binding at the DA transporter than the original GBR 12909 molecule, 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3- phenylpropyl)piperidine.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H15231N – PubChem