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Disclosed are a compound having cardiotonic activity and a pharmaceutical composition containing the same, and the composition containing the compound, according to the present invention, is useful for preventing and treating heart failure.COPYRIGHT KIPO 2016

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Piperidine – Wikipedia,
Piperidine | C5H9301N – PubChem

 

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The invention provides a compound of formula: or a salt thereof, wherein the variables RAA, n, ring A, ring B, R1a, R1b, R2, R3, R4, R5, R6, R7, R8, and R9 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

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Piperidine – Wikipedia,
Piperidine | C5H9267N – PubChem

 

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The present invention relates to methods of treating or preventing emesis in mammals, including humans, using an NK-1 antagonist in combination with one or more other active agents selected from (a) a glucocorticoid or corticosteroid, (b) a benzodiazepine, (c) metaclopramide and (d) an intracellular molecular scavenger.

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Reference:
Piperidine – Wikipedia,
Piperidine | C5H9259N – PubChem

 

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I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 3466-80-6, help many people in the next few years.Formula: C11H15N

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A Selenourea-Thiourea Br¡ãnsted Acid Catalyst Facilitates Asymmetric Conjugate Additions of Amines to alpha,beta-Unsaturated Esters

beta-Amino esters are obtained with high levels of enantioselectivity via the conjugate addition of cyclic amines to unactivated alpha,beta-unsaturated esters. A related strategy enables the kinetic resolution of racemic cyclic 2-arylamines, using benzyl acrylate as the resolving agent. Reactions are facilitated by an unprecedented selenourea-thiourea organocatalyst. As elucidated by DFT calculations and 13C kinetic isotope effect studies, the rate-limiting and enantiodetermining step of the reaction is the protonation of a zwitterionic intermediate by the catalyst. This represents a rare case in which a thiourea compound functions as an asymmetric Br¡ãnsted acid catalyst.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 3466-80-6, help many people in the next few years.Formula: C11H15N

Reference£º
Piperidine – Wikipedia,
Piperidine | C5H9308N – PubChem

 

Extended knowledge of 3466-80-6

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Discovery of novel bacterial elongation condensing enzyme inhibitors by virtual screening

The elongation condensing enzymes in the bacterial fatty acid biosynthesis pathway represent desirable targets for the design of novel, broad-spectrum antimicrobial agents. A series of substituted benzoxazolinones was identified in this study as a novel class of elongation condensing enzyme (FabB and FabF) inhibitors using a two-step virtual screening approach. Structure activity relationships were developed around the benzoxazolinone scaffold showing that N-substituted benzoxazolinones were most active. The benzoxazolinone scaffold has high chemical tractability making this chemotype suitable for further development of bacterial fatty acid synthesis inhibitors.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H9268N – PubChem

 

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Removal of the pyridine directing group from alpha-substituted N-(pyridin-2-yl)piperidines obtained via directed Ru-catalyzed sp3 C-H functionalization

Two strategies, “hydrogenation-hydride reduction” and “quaternization-hydride reduction”, are reported that make use of mild reaction conditions (room temperature) to efficiently remove the N-pyridin-2-yl directing group from a diverse set of C-2-substituted piperidines that were synthesized through directed Ru-catalyzed sp3 C-H functionalization. The deprotected products are obtained in moderate to good overall yields irrespective of the strategy followed, indicating that both methods are generally equally effective. Only in the case of 2,6-disubstituted piperidines, could the “quaternization-hydride reduction” strategy not be used. The “hydrogenation-hydride reduction” protocol was successfully applied to trans- and cis-2-methyl-N-(pyridin-2-yl)-6-undecylpiperidine in a short synthetic route toward (¡À)-solenopsin A (trans diastereoisomer) and (¡À)-isosolenopsin A (cis diastereoisomer). The absolute configuration of the enantiomers of these fire ant alkaloids could be determined via VCD spectroscopy.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H9248N – PubChem

 

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Substituted pyrazoles as hepatoselective HMG-CoA reductase inhibitors: Discovery of (3R,5R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl- benzylcarbamoyl)-2H-pyrazol-3-yl]-3,5-dihydroxyheptanoic acid (PF-3052334) as a candidate for the treatment of hypercholesterolemia

In light of accumulating evidence that aggressive LDL-lowering therapy may offer increased protection against coronary heart disease, we undertook the design and synthesis of a novel series of HMG-CoA reductase inhibitors based upon a substituted pyrazole template. Optimizing this series using both structure-based design and molecular property considerations afforded a class of highly efficacious and hepatoselective inhibitors resulting in the identification of (3R,5R)-7-[2-(4-fluoro-phenyl)-4-isopropyl-5-(4-methyl-benzyl- carbamoyl)-2H-pyrazol-3-yl]-3,5-dihydroxy-heptanoic (PF-3052334) as a candidate for the treatment of hypercholesterolemia.

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Piperidine – Wikipedia,
Piperidine | C5H9297N – PubChem

 

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Combined Imine Reductase and Amine Oxidase Catalyzed Deracemization of Nitrogen Heterocycles

A novel amine oxidase (AO)/imine reductase (IRED) system was developed for the deracemization of racemic amines. By combining (R)-6-hydroxy-d-nicotine oxidase (6-HDNO) with an (R)-IRED, a panel of racemic 2-substituted piperidines and pyrrolidines were deracemized to yield the (S)-amines in high yields and enantiomeric excess values. Other N-heterocycles were deracemized with monoamine oxidase (MAO-N) or 6-HDNO in combination with ammonia borane, which allowed comparison of the two enzyme deracemization approaches with that involving a chemical reducing agent.

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Piperidine – Wikipedia,
Piperidine | C5H9327N – PubChem

 

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Origins of Small Proton Chemical Shift Differences in Monodeuterated Methyl Groups

We have recently shown that the small proton chemical shift difference in 2-methyl-1-(methyl-d)piperidine supports a long-lived nuclear spin state. To identify additional candidate molecules with CH2D groups exhibiting accessible long-lived states, and to investigate the factors governing the magnitude of the shift differences, we report a computational and experimental investigation of methyl rotational equilibria and proton chemical shifts in a variety of 2-substituted 1-(methyl-d)piperidines. The polarity and size of the 2-substituent affect the 1,2-stereoisomeric relationship, and consequently, the strength of the rotational asymmetry within the CH2D group. Nonpolar and large 2-substituents prefer the equatorial position, and relatively large shift differences (i.e., > 13 ppb) are observed. Polar and small substituents, however, increasingly prefer the axial position, and medium to small shift differences (i.e., 0 to 9 ppb) are observed. In addition, the diastereotopic CH2D proton chemical shift difference for tricarbonyl(1-chloro-2-deuteriomethylbenzene) chromium(0) was computed, showing that reasonable predictions of these small shift differences can be extended to more complex, organometallic species.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H9245N – PubChem

 

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3466-80-6 2-Phenylpiperidine 103020, apiperidines compound, is more and more widely used in various.

3466-80-6, 2-Phenylpiperidine is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

3-Chloro-4-hydroxybenzoic Acid {2-Methoxy-4-[2-(2-phenylpiperidin-1-yl)ethoxy]benzylidene}hydrazide This compound was prepared analogously to the compound described in the previous example starting from resin bound 3-chloro-4-hydroxybenzoic acid hydrazide (resin-[building block 1]) (2 g, ~2 mmoles), 4-(2-bromoethoxy)-2-methoxybenzaldehyde ([building block 2]) (0.73 g, 1.5 equivs.), and 2-phenylpiperidine ([building block 3]) (3.0 g, 10 equivs.). After cleavage with 50% trifluoroacetic acid, the residue (1.0 g) was purified by column chromatography on silica gel (28 g) eluding with a mixture of methanol and dichloromethane (1:13). This afforded 0.24 g of the title compound. 1H-NMR (400 MHz, DMSO-d6): deltaH=1.4 (2H, m), 1.65 (4H, m), 2.25 (2H, m), 2.75 (1H, m), 3.16 (1H, d), 3.25 (2H, d), 3.83 (3H, s), 4.0 (2H, m), 6.50 (1H, d), 6.54 (1H, s), 7.07 (1H, d), 7.23 (1H, t), 7.35 (4H, m), 7.73 (1H, d), 7.77 (1H, dd), 7.96 (1H, d), 8.65 (1H, s), 10.9 (1H, s), 11.6 (1H, s).

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Reference£º
Patent; Novo Nordisk A/S; US6613942; (2003); B1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem