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Topic: Piperidine


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PCP

  
 [No title]   (Site not responding. Last check: 2007-10-22)
PIPERIDINE The invention relates to an improved process for the hydrogenation of pyridine compounds to produce piperidine compounds.
Also, it is desirable to use a hydrogenation catalyst that is not costly and can be used to produce a sufficient quantity of piperidine compounds per quantity of pyridine compounds such that the cost of the hydrogenation catalyst is low compared to the other costs associated with the hydrogenation process.
The thus-activated hydrogenation catalyst can be used in the hydrogenation of pyridine compounds to piperidine compounds by contacting, under conversion conditions, a hydrocarbon feedstock comprising at least one pyridine compound with the inventive activated hydrogenation catalyst.
www.wipo.int /cgi-pct/guest/getbykey5?KEY=00/73291.001207&ELEMENT_SET=DECL   (4541 words)

  
 Pyrrolidine, Tropane, Piperidine and Polyketide Alkaloids   (Site not responding. Last check: 2007-10-22)
The pungent compounds in fl pepper are piperidine units that have interacted with phenylpropanoid compounds.
Piperidine alkaloids with portions derived from malonyl-CoA and phenylalanine
This alkaloid is similar in structure to piperidine alkaloids, but is derived from polyketide pathways.
www.life.uiuc.edu /plantbio/363/lecture29.html   (642 words)

  
 Spectrum Laboratories : Chemical Fact Sheet - Cas # 110894
Inhalation of 2.9 ppm piperidine 4 hr/day for 4 mo caused altered spermatogenesis in rats.
Piperidine was not carcinogenic in the A mouse pulmonary tumor system and no DNA damage was found in an alkaline elution/rat hepatocyte assay.
ARTS: Piperidine is used as a solvent and chemical intermediate, as a curing agent for rubber and epoxy chemical resins, a catalyst for condensation reactions, an ingredient in oils and fuels, and a complexing agent(1).
www.speclab.com /compound/c110894.htm   (2229 words)

  
 PIPERIDINE ALKALOIDS
Piperidine alkaloids are identified by their saturated heterocyclic ring, i.e., piperidine nucleus.
The best known piperidine alkaloid poisons are those of poison hemlock, Conium maculatum.
Socrates is reputed to have been killed with a poison hemlock extract.
www.ansci.cornell.edu /plants/toxicagents/piperidi.html   (510 words)

  
 JIAS:Volume 5/4   (Site not responding. Last check: 2007-10-22)
Piperidine is among the most important heterocyclic compounds which exhibits its therapeutic activity due to its conformationally flexible nature.
The accentuated interest in the piperidine class of opiate analgesics continues to be expressed in the pharmaceutical community; the synthesis and biological properties of these agents have been the subject of on going investigations (1).
However when the methyl group is displaced from the nitrogen atom of the piperidine to that of phenacyl function, resulted in decrease in analgesic activity.
www.medicaljournal-ias.org /5_4/Hameed.htm   (1214 words)

  
 Piperidine derivatives and hypotensives containing the same - Patent 5393890
The piperidine compound of claim 1, wherein Q is substituted or unsubstituted piperidinyl.
The present piperidine derivative may be prepared in the form of ordinary preparations such as for example, tablets, powders, capsules, solutions, sugar--coated tablets or depots, which may be prepared in a conventional manner using conventional preparation aids.
From the foregoing results, it is understood that the piperidine derivatives of the present invention possess hypotensive activity and are usable as hypotensives and therefore, they can be expected to provide an excellent hypotensive effect.
www.freepatentsonline.com /5393890.html   (1795 words)

  
 From Peptides to Non-Peptide Peptidomimetics: Design and Synthesis of New Piperidine Inhibitors of Aspartic Peptidases
These piperidines can be designed from peptide-derived inhibitors by use of a structure-generating program but only after the enzyme active site conformation has been modified in a mechanistically related fashion.
The discovery of these piperidines as a new class of aspartic peptidase inhibitor represents a major advance in the design of inhibitors.
The binding of the piperidine nitrogen to the enzyme catalytic carboxyl groups is similar to the binding of the statine hydroxyl
pubs.acs.org /cgi-bin/jtextd?orlef7/3/i15/html/ol016092u.html   (2356 words)

  
 Common Degradative Pathways of Morpholine, Thiomorpholine, and Piperidine by Mycobacterium aurum MO1: Evidence from ...
Piperidine was exhausted after 3 h of incubation.
Degradation of morpholine, piperidine, and pyrrolidine by mycobacteria: evidences for the involvement of a cytochrome P450.
Cloning and characterization of the genes encoding a cytochrome P450 (PipA) involved in piperidine and pyrrolidine utilization and its regulatory protein (PipR) in Mycobacterium smegmatis mc2155.
aem.asm.org /cgi/content/full/66/8/3187   (3343 words)

  
 : Let's Take a Peek at the PEAC software   (Site not responding. Last check: 2007-10-22)
There is no established IDLH for Piperidine but the Department of Energy’s Emergency Management Advisory Committee’s Subcommittee on Consequence Assessment and Protective Action (SCAPA) has developed a TEEL-(1,2,3) (Temporary Emergency Exposure Limit) as a temporary substitute for the ERPGs through a formulaic derivation.
Piperidine has a relatively low vapor pressure (30 mm Hg), so if a small amount is spilled and forms a puddle, the amount of vapor released is very minimal.
For our scenario using Piperidine as the spilled chemical we’ll use Salt Lake City as the location and the time as 2:30 AM on January 16th.
www.imakenews.com /aristatek/e_article000122651.cfm   (1343 words)

  
 eMedicine - Toxicity, Antihistamine : Article by Brett Roth, MD   (Site not responding. Last check: 2007-10-22)
Piperidine derivatives generally have a prolonged duration of action and low incidence of drowsiness.
Piperidine derivatives (eg, terfenadine, astemizole, loratadine) are peripherally selective H1 antagonists with few GI adverse effects and a low incidence of drowsiness (see Nonsedating antihistamines).
Phenothiazines, diphenhydramine, and the nonsedating piperidine antihistamines are associated with prolongation of the QT interval.
www.emedicine.com /emerg/topic38.htm   (4778 words)

  
 Synthesis of enantiopure pyrrolidine and piperidine derivatives   (Site not responding. Last check: 2007-10-22)
Synthetic approaches to enantiopure 5- and 6-membered azaheterocycles have elicited a great deal of recent interest, because of their potential use as valuable intermediates for the synthesis of complex organic molecules.
Several of these functionalized pyrrolidines and piperidines have been shown recently to exhibit diverse biological activities, especia- lly as excellent glycosidase inhibitors.
Furthermore, chiral 2-substituted pyrrolidines and piperidines occur as natural products and are useful as chiral bases, chiral auxiliaries, and chiral ligands.
www.weizmann.ac.il /ICS/chemistry66/054Kumareswaran.html   (184 words)

  
 N-[1-(2-Benzo[b]Thiophenyl)Cyclohexyl]- Piperidine (BTCP) Exerts Cocaine-Like Actions on Drug-Maintained Responding in ...   (Site not responding. Last check: 2007-10-22)
The effects of N-[1-(2-benzo[b]thiophenyl)cyclohexyl]- piperidine (BTCP), a phencyclidine derivative that acts as a potent dopamine reuptake inhibitor, were examined on cocaine self-administration in rats.
It is widely accepted that the addictive and reinforcing actions of cocaine are the result of the drug's ability to block the reuptake of dopamine (DA) by inhibiting the dopamine transporter (DAT) and, thereby, increasing DA neurotransmission (Kuhar 1992; Ritz et al.
N-[1-(2-benzo[b]thiophenyl)cyclohexyl] piperidine (BTCP) is a phencyclidine (PCP) derivative that has high affinity for the DAT (Chaudieu et al.
www.nature.com /cgi-taf/dynapage.taf?file=/npp/journal/v23/n3/full/1395512a.html   (6459 words)

  
 Environmental Protection Agency
Warning: Piperidine is a basic irritant of skin and mucous membranes.
Signs and symptoms of acute exposure to piperidine may include irritation and burning of skin and mucous membranes.
Acute exposure to piperidine may require decontamination and life support for the victims.
yosemite.epa.gov /oswer/CeppoEHS.nsf/firstaid/110-89-4?OpenDocument   (545 words)

  
 Further SAR Studies of Piperidine-Based Analogues of Cocaine. 2. Potent Dopamine and Serotonin Reuptake Inhibitors
All members of this series were prepared from arecoline hydrobromide in optically pure form and were evaluated for their ability to inhibit high affinity uptake of dopamine (DA), serotonin (5-HT) and norepinephrine (NE) into rat brain nerve endings (synaptosomes).
As is apparent from the data presented, the naphthyl substituted piperidines 6-9, which differ in their stereochemistry, show different degrees of selectivity for the three transporters.
Despite its 2.5-fold greater DAT activity compared to cocaine, piperidine 14 was found to be about 2.5-fold less potent in increasing distance traveled in mice.
pubs.acs.org /cgi-bin/abstract.cgi/jmcmar/2000/43/i06/abs/jm9905561.html   (400 words)

  
 Quinolylpropylpiperidine derivatives, their preparation and the compositions which comprise them - Patent 6403610
The conversion of the hydroxymethyl radical in the 3-position of the piperidine to a 2-carboxyethyl radical is carried out, for example, from the halogenated derivative prepared as described above by condensation of the sodium salt of diethyl malonate, followed by acid hydrolysis in aqueous medium of the product obtained.
The intermediates of the quinolylpropylpiperidine derivatives in which R.sub.4 represents alkenyl-CH.sub.2 O-- or alkynyl-CH.sub.2 O-- can be obtained, by analogy with the preparation of the intermediates in which R.sub.4 is alkyloxy, by the action of the corresponding halogenated derivative on the quinoline derivative hydroxylated in the 6-position.
The derivatives with the trans configuration can be obtained from the derivatives with the cis configuration according to or by analogy with the method disclosed in International Application WO 99/37635, the disclosure of which is specifically incorporated by reference herein.
www.freepatentsonline.com /6403610.html   (5862 words)

  
 Piperidine derivatives and process for their production (US5994549)   (Site not responding. Last check: 2007-10-22)
A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents.
A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.
K.Y. Chan, et al., "Direct enantiomeric separation of terfenadine and its major acid metabolite by high-performance liquid chromatography, and the lack of stereoselective terfenadine enantiomer biotransformation in man," Journal of Chromatography, 271:291-97 (1991).
www.delphion.com /details?pn=US05994549__   (1111 words)

  
 Endogenous Activation of Serotonin-2A Receptors Is Required for Respiratory Rhythm Generation In Vitro -- Peña ...
The effect of ketanserine is similar to the effect of two other 5-HT antagonists, piperidine (B) and spiperone (C), but not to the effect of the specific 5-HT antagonist SB206553 (D), which has no effect on the fictive respiratory activity.
Note that the PKC activator abolished the depression in population activity and the discharge pattern of the inspiratory neuron produced by piperidine (B).
Note that the duration of the burst is reduced and the amplitude is increased after the application of piperidine.
www.jneurosci.org /cgi/content/full/22/24/11055   (6648 words)

  
 [No title]   (Site not responding. Last check: 2007-10-22)
The word "piperidine" is peppered throughout UNODC descriptions of the pethidine group of drugs.
The piperidine group is a 6 membered ring, with 5 carbons and an NH group.
At the time the UNODC document was being bounced around through cyberspace no experts in psychopharmacology were on hand to sharpen the public's piperidine inquiry.
www.paxilprotest.com /page22.html   (595 words)

  
 Cloning and Characterization of the Genes Encoding a Cytochrome P450 (PipA) Involved in Piperidine and Pyrrolidine ...
Cloning and Characterization of the Genes Encoding a Cytochrome P450 (PipA) Involved in Piperidine and Pyrrolidine Utilization and Its Regulatory Protein (PipR) in Mycobacterium smegmatis mc2155 -- Poupin et al.
The piperidine and pyrrolidine concentrations were estimated spectrophotometrically by the method of Stevens and Skov (49)
Cloning of the gene encoding a regulatory protein of the piperidine metabolism pathway.
jb.asm.org /cgi/content/full/181/11/3419   (4340 words)

  
 ARS | Publication request: Plant Alkaloids: Piperidine, Pyridine, Quinolizidine, Steroidal Alkaloids   (Site not responding. Last check: 2007-10-22)
Interpretive Summary: The series of short articles provides a comprehensive review for the reference text, "Clinical Veterinary Toxicology." The subject matter is an invited contribution whereby the source, toxicokinetics, mechanism of action, toxicity and risk factors, clinical signs, clinical pathology/lesions, diagnostic testing, treatment/prognosis, and prevention and control of selected poisonous plants is discussed.
The specific poisonous plants include selected species containing the piperidine, pyridine, quinolizidine and Veratrum-type steroidal alkaloids.
Technical Abstract: The series of short articles provides a comprehensive review for the reference text, "Clinical Veterinary Toxicology." The subject matter is an invited contribution whereby the source, toxicokinetics, mechanism of action, toxicity and risk factors, clinical signs, clinical pathology/lesions, diagnostic testing, treatment/prognosis, and prevention and control of selected poisonous plants is discussed.
www.ars.usda.gov /research/publications/publications.htm?SEQ_NO_115=119547&pf=1   (208 words)

  
 Search Results for piperidine - Encyclopædia Britannica
hallucinogenic drug with anesthetic properties, having the chemical name 1–(1–phencyclohexyl) piperidine.
PCP was first developed in 1956 by Parke Davis Laboratories of Detroit, Mich., for use as an...
Expand your search on piperidine with these databases:
www.britannica.com /search?query=piperidine&submit=Find&source=MWTAB   (170 words)

  
 Eugene Applebaum College of Pharmacy and Health Sciences
Expansion of Structure Activity Studies in piperidine analogs of GBR compounds by altering substitutions in the N-benzyl moiety.
Design, synthesis, and activity of novel cis- and trans-3,6-disubstituted pyran biomimetics of 3,6-disubstituted piperidine as potential ligand for the dopamine transporter.
High affinity hydroxy piperidine analogues of 4-(2-benzhydryloxyethyl)-1-(4-fluorobenzyl)piperidine for the dopamine transporter:Stereospecific interactions in vitro and in vivo.
www.cphs.wayne.edu /PSC/dutta/publications.html   (689 words)

  
 Better Mosquito, Tick Repellents in the Wind? / January 3, 2002 / News from the USDA Agricultural Research Service   (Site not responding. Last check: 2007-10-22)
The original repellent, called 220 for short, is based on piperidine, a hexagonally- shaped molecule found in trace amounts in fl pepper.
Two other chemical groups are attached to this hexagon, but each can attach at two different angles.
Other chemical groups can attach to the piperidine scaffold at various locations and angles, yielding dozens of candidates for testing, according to Klun, at ARS’ Chemicals Affecting Insect Behavior Laboratory in Beltsville, Md.
www.ars.usda.gov /is/pr/2002/020103.htm   (359 words)

  
 Fentanyl Metabolism by Human Hepatic and Intestinal Cytochrome P450 3A4: Implications for Interindividual Variability ...
N-benzyl-4-anilino piperidine (A): N-benzyl-4-piperidone (3.7 ml, 0.02 mole) was dissolved in anhydrous toluene (20 ml).
GC-MS: m/z 91 (---CH norfentanyl (C): N-benzyl-4-propylanilido piperidine (B) (30 mg) was dissolved in 2 ml of 50% ethanol/water.
The third objective was to determine whether metabolic biotransformation of fentanyl occurs in human duodenal microsomes.
dmd.aspetjournals.org /cgi/content/full/25/9/1072   (5251 words)

  
 ketamine   (Site not responding. Last check: 2007-10-22)
Both piperidine and cyclohexane rings are in the chair conformation.
The protonated piperidine retains the chair conformation with the phenyl group equatorial.
If the piperidine ring remains protonated at the PCP receptor site, there is a significant chance that binding is occuring through the conformation shown in scenario #3 with protonated piperidine in the boat conformation.
www.pitt.edu /~soriano/models/ketamine/ketamine.html   (709 words)

  
 Studies on the synthesis of Strychnos indole alkaloids from 2-(3-indolyl)piperidine derivatives.   (Site not responding. Last check: 2007-10-22)
The attempted elaboration of the pentacyclic skeleton of Strychnos indole alkaloids by a Pummerer-initiated sequential closure of C and E rings from a 2-(3-indolyl)piperidine-4-acetate derivative bearing a 2-(phenylsulfinyl)ethyl chain on the piperidine nitrogen is described.
An indolo[3,2-a]quinolizidine, resulting from the direct attack of the intermediate thionium ion on the 2 position of the heterocycle, is obtained instead.
Thus, compound 4 was treated with 2-iodoethyl phenyl sulfide and the resulting pyridinium salt was subsequently reduced with sodium borohydride to give the desired tetrahydropyridine 9 as a mixture of stereoisomers (Scheme 2).
www.arkat-usa.org /ark/journal/2004/I04_Melendez/EM-755K/755K.asp   (3629 words)

  
 Eugene Applebaum College of Pharmacy and Health Sciences
Madras B.K, Reith M.E.A, Meltzer P.C, Dutta A.K. “O-526, A piperidine analog of GBR 12909, retains high affinity for the dopamine transporter in monkey caudate-putamen”.
Dutta A K, Davis M, Fei X-S, Beardsley P. M, Cook C D, Reith M. Expansion of Structure-Activity Studies in piperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (GBR 12935) compounds by altering substitutions in the N-benzyl moiety and behavioral pharmacology of selected molecules.
Zhang S, Reith M E A, Dutta A K. Design, synthesis, and activity of novel cis- and trans-3,6-disubstituted pyran biomimetics of 3,6-disubstituted piperidine as potential ligands for the dopamine transporter.
wizard.pharm.wayne.edu /psc/faculty/dutta/allpubs.html   (1222 words)

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