Category: piperidines

B(C₆F₅)₃-Catalyzed C-H Alkylation of N-Alkylamines Using Silicon Enolates without External Oxidant was written by Chan, Jessica Z.;Chang, Yejin;Wasa, Masayuki. And the article was included in Organic Letters in 2019.Quality Control of 1,2,2,6,6-Pentamethylpiperidine This article mentions the following:

An efficient method for the coupling of N-alkylamines with silicon enolates to generate 尾-amino carbonyl compounds is disclosed. These reactions proceed by activation of 伪-amino C-H bonds by B(C₆F₅)₃, which likely generates a “frustrated” acid/base complex in the presence of large N-alkylamines. The transformation requires no external oxidant and releases hydrosilane as a byproduct. The utility of this method is demonstrated in the late-stage functionalization of bioactive mols. such as citalopram, atomoxetine, and fluoxetine. In the experiment, the researchers used many compounds, for example, 1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0Quality Control of 1,2,2,6,6-Pentamethylpiperidine).

1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Quality Control of 1,2,2,6,6-Pentamethylpiperidine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Evidence for multiple alkali metal cation complexation in membrane-spanning ion transporters was written by Shabany, Hossein;Murray, Clare L.;Gokel, George W.;Gloeckner, Charles A.;Grayson, Michael A.;Gross, Michael L.. And the article was included in Chemical Communications (Cambridge) in 2000.Application of 15336-72-8 This article mentions the following:

The polynitrogen-containing cation transporters 1-4 are shown by electrospray mass spectrometry to form multi-cationic species. In the absence of Na⁺, protonated species dominate but increasing the sodium concentration leads to all binding sites being occupied. In the experiment, the researchers used many compounds, for example, 4,4′-Bipiperidine (cas: 15336-72-8Application of 15336-72-8).

4,4′-Bipiperidine (cas: 15336-72-8) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N鈥揌 bond in an axial position, and the other in an equatorial position.Application of 15336-72-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis of fused dihydropyrido[e]purines via ring closing metathesis was written by Litinas, Konstantinos E.;Thalassitis, Andreas. And the article was included in Tetrahedron Letters in 2010.Application In Synthesis of 6-(Piperidin-1-yl)-9H-purine This article mentions the following:

Ring closing metathesis (RCM) of 8,9-diallylpurines or 9-butenyl-8-vinylpurines with the Grubbs 2nd generation catalyst resulted in fused 6,9- or 8,9-dihydropyrido[e]purines, resp. The 8,9-dialkenylpurines were prepared from 8-bromopurines after 9-alkenylation and subsequent Stille coupling at C-8 with alkenylstannanes in the presence of Pd(PPh₃)₄ or Pd(PPh₃)₂Cl₂. In the experiment, the researchers used many compounds, for example, 6-(Piperidin-1-yl)-9H-purine (cas: 1928-81-0Application In Synthesis of 6-(Piperidin-1-yl)-9H-purine).

6-(Piperidin-1-yl)-9H-purine (cas: 1928-81-0) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Application In Synthesis of 6-(Piperidin-1-yl)-9H-purine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Intensified fish farming. Performance of electrochemical remediation of marine RAS waters was written by Santos, German;Ortiz-Gandara, Isabel;Del Castillo, Andres;Arruti, Axel;Gomez, Pedro;Ibanez, Raquel;Urtiaga, Ane;Ortiz, Inmaculada. And the article was included in Science of the Total Environment in 2022.Safety of 4-Oxo-tempo This article mentions the following:

Aquaculture has been the fastest growing agricultural sector in the past few decades and currently supplies about half of the fish market. A range of environmental and management concerns including limited land and water availability have led to intensifying fish production by recirculating aquaculture systems (RAS). Fish鈥瞫 diet contains 30-60 % protein and about 4-10 % nitrogen (N). As fish assimilate only 20-30 % of the feed to produce body mass, the unassimilated N is released in the form of toxic ammonium that deteriorates water quality and compels its degradation Widely extended biol. nitrification is not efficient in the removal of nitrites nor other chems. and pharmaceuticals used during fish culture. Electrochem. oxidation, a less developed alternative, reports several advantages such as, i) simultaneous degradation of ammonia-nitrogen (TAN) and water disinfection in the same step with considerable simplification of the whole process, ii) easy adaptability to different production scales and periods of fish growth, and iii) no generation of harmful byproducts and no use of chems., among others. Besides, in the case of marine aquaculture, the technol. benefits from the high conductivity of seawater; thus, electrochem. oxidation is positioned in a very good place to satisfy the water treatment needs of the increasing production rate of marine aquaculture fish. Here, we report the anal. of the performance of a RAS demonstration plant aimed at farming gilthead sea bream (Sparus aurata) and sea bass (Dicentrarchus labrax) and provided with electrochem. remediation of culture water. The performance of the plant, with 20 m³ of seawater operating at a recirculation rate of 0.9-1.4 h^-1, has been analyzed in terms of TAN removal, water disinfection, make-up water intake and energy consumption and compared to data of conventional RAS provided with biofilters. The benefits and advantages of the innovative electrochem. remediation of RAS water are highlighted. In the experiment, the researchers used many compounds, for example, 4-Oxo-tempo (cas: 2896-70-0Safety of 4-Oxo-tempo).

4-Oxo-tempo (cas: 2896-70-0) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Safety of 4-Oxo-tempo

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Detailed Exploration around 4-Aminoquinolines Chemical Space to Navigate the Lysine Methyltransferase G9a and DNA Methyltransferase Biological Spaces was written by Rabal, Obdulia;Sanchez-Arias, Juan Antonio;San Jose-Eneriz, Edurne;Agirre, Xabier;de Miguel, Irene;Garate, Leire;Miranda, Estibaliz;Saez, Elena;Roa, Sergio;Martinez-Climent, Jose Angel;Liu, Yingying;Wu, Wei;Xu, Musheng;Prosper, Felipe;Oyarzabal, Julen. And the article was included in Journal of Medicinal Chemistry in 2018.Recommanded Product: 144222-22-0 This article mentions the following:

Epigenetic regulators that exhibit aberrant enzymic activities or expression profiles are potential therapeutic targets for cancers. Specifically, enzymes responsible for methylation at histone-3 lysine-9 (like G9a) and aberrant DNA hypermethylation (DNMTs) have been implicated in a number of cancers. Recently, mols. bearing a 4-aminoquinoline scaffold were reported as dual inhibitors of these targets and showed a significant in-vivo efficacy in animal models of hematol. malignancies. Here, we report a detailed exploration around three growing vectors born by this chemotype. Exploring this chem. space led to the identification of features to navigate G9a and DNMT1 biol. spaces; not only their corresponding exclusive areas, selective compounds, but also common spaces. Thus, we identified from selective G9a and first-in-class DNMT1 inhibitors, > 1 log unit between their IC₅₀ values, with IC₅₀ < 25nM (e.g. 43 and 26, resp.) to equipotent inhibitors with IC₅₀ < 50nM for both targets (e.g. 13). Their ADME/Tox profiling and antiproliferative efficacies, vs. some cancer cell lines, are also reported. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0Recommanded Product: 144222-22-0).

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Recommanded Product: 144222-22-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Neutral Molecule Receptor Systems Using Ferrocene’s “Atomic Ball Bearing” Character as the Flexible Element was written by Li, Chensheng;Medina, Julio C.;Maguire, Glenn E. M.;Abel, Ernesto;Atwood, Jerry L.;Gokel, George W.. And the article was included in Journal of the American Chemical Society in 1997.Application of 15336-72-8 This article mentions the following:

Fourteen novel ferrocene derivatives were designed to serve as receptors for low mol. weight diamines. The compounds that were prepared and fully characterized possess two ferrocenedicarboxylic acid residues bridged by amide formation in their resp. 1′-positions by 4,4′-benzidinyl (15), 3,3′-dimethoxy-4,4′-benzidinyl (16), 2,7-fluorenyl (17), 3-methoxy-2,7-fluorenyl (18), 4-N-piperazinoanilinyl (19), N,N’-4,4′-bipiperdinyl (20; shown as I), and 4,13-diaza-18-crown-6 (21). In two cases, ferrocenecarboxylic acid was bridged by spacers attached using 1-methylene groups. The bridges in these cases were 4,13-diaza-18-crown-6 (22) and 1,5-diaminoanthraquinone (24). In a single case, ferrocenecarboxylic acid was bridged by 1,5-dicarbonylnaphthalene (25). In one addnl. case, the bridge was created by formation of an imine followed by hydrogenation, but both compounds proved to be relatively unstable. Attempts to increase solubility afforded the N-ethylated derivative of 15 and the derivative 27 having carboxamides in the 1′-positions. A solid state structure of the di-Et ester of 20 confirms the design criteria. Complexation constants were determined in THF-d₈ or CDCl₃ for combinations of receptors 18, 19, and 20 with 4-aminopyridine, N,N,N’,N’-tetramethylethylenediamine, N,N,N’,N’-tetramethylpropylenediamine, DABCO, 3-propyladenine, and benzimidazole and were in the range 10²-10⁴. The anticipated complexation mechanism for 20 with N,N,N’,N’-tetramethylpropylenediamine was confirmed by observation of an NOE between host and guest. In the experiment, the researchers used many compounds, for example, 4,4′-Bipiperidine (cas: 15336-72-8Application of 15336-72-8).

4,4′-Bipiperidine (cas: 15336-72-8) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Application of 15336-72-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

New gradient high-performance liquid chromatography method for determination of donepezil hydrochloride assay and impurities content in oral pharmaceutical formulation was written by Kafkala, Stella;Matthaiou, Stella;Alexaki, Pandora;Abatzis, Morfis;Bartzeliotis, Antonios;Katsiabani, Maria. And the article was included in Journal of Chromatography A in 2008.HPLC of Formula: 120014-30-4 This article mentions the following:

A new gradient HPLC method has been developed and validated for the determination of both assay and related substances of donepezil hydrochloride in oral pharmaceutical formulation. Different kinds of columns and gradient elution programs were tested in order to achieve satisfactory separation between the active substance, 4 impurities and an interfering excipient used in the formulation. Best results were obtained using an Uptisphere ODB C₁₈ column 250 mm 脳 4.6 mm, 5 渭m, UV detection at 270 nm and a gradient elution of phosphate buffer (0.005M, pH 3.67) and methanol as the mobile phase. The method was validated with respect to linearity, precision, accuracy, specificity and robustness. It was also a stability-indicating method, and therefore suitable for the routine anal. of donepezil and related substances in the pharmaceutical formulation. In the experiment, the researchers used many compounds, for example, 5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one (cas: 120014-30-4HPLC of Formula: 120014-30-4).

5,6-Dimethoxy-2-(piperidin-4-ylmethyl)-2,3-dihydro-1H-inden-1-one (cas: 120014-30-4) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.HPLC of Formula: 120014-30-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Solubility of Racemic Paroxetine Intermediate in Supercritical Carbon Dioxide was written by Bao, Zong-Bi;Wei, Zuo-Jun;Su, Bao-Gen;Ren, Qi-Long. And the article was included in Journal of Chemical & Engineering Data in 2006.SDS of cas: 109887-53-8 This article mentions the following:

The solubility of racemic paroxetine intermediate in supercritical carbon dioxide was measured in the pressure range from (9 to 24) MPa and at temperatures of (308.2, 318.2, and 328.2) K using a continuous flow-type apparatus equipped with a high-pressure UV-Vis detector. Results showed that under the present operation conditions, the exptl. determined solubility of the racemic compound was in the range of (7.3 脳 10^-5 to 1.2 脳 10^-3) in mole fraction. The solubility increased with rising pressure at constant temperature, and the crossover pressure was found to locate at around 12 MPa for the three solubility isotherms. An empirical d.-based Chrastil’s equation was used to fit the exptl. solubility data, giving a good correlation with an AARD of 7.56 %. In the experiment, the researchers used many compounds, for example, ((3R,4S)-rel-4-(4-Fluorophenyl)-1-methylpiperidin-3-yl)methanol (cas: 109887-53-8SDS of cas: 109887-53-8).

((3R,4S)-rel-4-(4-Fluorophenyl)-1-methylpiperidin-3-yl)methanol (cas: 109887-53-8) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.SDS of cas: 109887-53-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Design and development of oral thin film of antihistaminic drug fexofenidine was written by Shrivas, Astha;Jain, Ashish;Yadav, Pradeep Kumar;Singhai, Akhlesh Kumar. And the article was included in World Journal of Pharmaceutical Research in 2022.Recommanded Product: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid hydrochloride This article mentions the following:

Bioadhesive formulations have a wide scope of applications, for both systemic and local effects. The mucosa is relatively permeable with a rich blood supply. The oral transmucosal drug delivery bypasses first pass effect and avoids pre-systemic elimination in the GI tract. These factors make the oral mucosa a very attractive and feasible site for systemic drug delivery. A few drugs have been successfully administered via buccal route. The buccal region offers an attractive route of administration for systemic drug delivery. Fexofenadine, H1 antagonist, is a potent antihistamine. Buccal absorption studies of fexofenadine having partition coefficient less than 2 and have lipophilicity in nature, which offers advantages of buccal route over oral route. By observing the above points, it is inferred that fexofenadine has a need to formulate into buccal patches and the drug is suitable for it. Bioadhesive formulations have a wide scope of applications, for both systemic and local effect for management of diseases. Fexofenadine drug will be use for developing a dosage form for a very quick onset of action, which is beneficial in managing severe conditions of allergies, aiding in the enhancement of bioavailability, and is very convenient for administration, without the problem of swallowing and using water. In the present study, Fexofenadine HCl was used as a model drug candidate and nine fast-dissolving films formulations containing different polymer concentrations were prepared Fast-dissolving films of Fexofenadine HCl were prepared by the solvent casting method on glass molds, using HPMC E15 and Xanthan gum, Sodium starch glycolate as disintegrating agent, glycerin as plasticizer and aspartame as sweetener and distilled water as a solvent. The effect of the nature of polymers was studied by preparing various formulations of oral dispersible films. The various formulations containing a combination of polymers, release was found to be in the following order: OTF7 > OTF8 > OTF9 and formulations OTF7, OTF1, and OTF4 were found to be the best formulations in terms of drug release. The results of the release kinetics study showed that all the formulations obeyed first order drug release profile more closely, i.e., the release rate depended upon the initial concentration of drug. The slope values of the Korsmeyer-Peppas plot showed that the mechanism was non-fickian or supercase II transport mechanism. In the experiment, the researchers used many compounds, for example, 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid hydrochloride (cas: 153439-40-8Recommanded Product: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid hydrochloride).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid hydrochloride (cas: 153439-40-8) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Recommanded Product: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Mesogenic esters of the 4-(alkylpiperidino) benzoic acids was written by Adomenas, P.;Sirutkaitis, R.. And the article was included in Molecular Crystals and Liquid Crystals in 1985.Product Details of 97096-92-9 This article mentions the following:

A number of 4-(4-alkylpiperidino)benzoic acids, alkyl 4-(4-alkylpiperidino)benzoates, and aryl 4-(4-alkylpiperidino)benzoates were prepared and their properties were examined (especially liquid crystal properties). In the experiment, the researchers used many compounds, for example, 4-(4-Methylpiperidin-1-yl)benzoic acid (cas: 97096-92-9Product Details of 97096-92-9).

4-(4-Methylpiperidin-1-yl)benzoic acid (cas: 97096-92-9) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Product Details of 97096-92-9

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem