Day: October 18, 2022

《Design, synthesis and biological activities of piperidine-spirooxadiazole derivatives as α7 nicotinic receptor antagonists》 was published in European Journal of Medicinal Chemistry in 2020. These research results belong to Zhang, Han; He, Xiaomeng; Wang, Xintong; Yu, Bo; Zhao, Siqi; Jiao, Peili; Jin, Hongwei; Liu, Zhenming; Wang, KeWei; Zhang, Liangren; Zhang, Lihe. Category: piperidines The article mentions the following:

7 Nicotinic acetylcholine receptors (nAChRs) expressed in the nervous and immune systems was suggested to play important roles in the control of inflammation. However, the lack of antagonist tools specifically inhibiting α7 nAChR impedes the validation of the channel as therapeutic target. To discover a selective α7 antagonist, a pharmacophore-based virtual screening and identified a piperidine-spirooxadiazole derivative T761-0184 that acts as a α7 antagonist. A series of novel piperidine-spirooxadiazole derivatives were subsequently synthesized and evaluated using two-electrode voltage clamp (TEVC) assay in Xenopus oocytes. Lead compounds from two series inhibited α7 with their IC50 values ranging from 3.3μM to 13.7μM. Compound 3-(4-Bromophenyl)-8-methyl-1-oxa-2,4,8-triazaspiro[4.5]dec-2-ene exhibited α7 selectivity over other α4β2 and α3β4 nAChR subtypes. The anal. of structure-activity relationship (SAR) provides valuable insights for further development of selective α7 nAChR antagonists. In the experiment, the researchers used 1-Methyl-4-piperidone(cas: 1445-73-4Category: piperidines)

1-Methyl-4-piperidone(cas: 1445-73-4) is a member of piperidine. Piperidine is ubiquitous structural motif widely occurred in diverse synthetically and naturally occurring bioactive molecules. Piperidines are an immensely important class of compounds medicinally: the piperidine ring is the most common heterocyclic subunit among FDA approved drugs.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Discovery of Reversible Inhibitors of KDM1A Efficacious in Acute Myeloid Leukemia Models》 was written by Romussi, Alessia; Cappa, Anna; Vianello, Paola; Brambillasca, Silvia; Cera, Maria Rosaria; Dal Zuffo, Roberto; Faga, Giovanni; Fattori, Raimondo; Moretti, Loris; Trifiro, Paolo; Villa, Manuela; Vultaggio, Stefania; Cecatiello, Valentina; Pasqualato, Sebastiano; Dondio, Giulio; So, Chi Wai Eric; Minucci, Saverio; Sartori, Luca; Varasi, Mario; Mercurio, Ciro. HPLC of Formula: 109384-19-2 And the article was included in ACS Medicinal Chemistry Letters in 2020. The article conveys some information:

Lysine-specific demethylase 1 (LSD1 or KDM1A) is a FAD-dependent enzyme that acts as a transcription corepressor or coactivator by regulating the methylation status of histone H3 lysines K4 and K9, resp. KDM1A represents an attractive target for cancer therapy. While, in the past, the main medicinal chem. strategy toward KDM1A inhibition was based on the optimization of ligands that irreversibly bind the FAD cofactor within the enzyme catalytic site, we and others have also identified reversible inhibitors. Herein we reported the discovery of 5-imidazolylthieno[3,2-b]pyrroles, a new series of KDM1A inhibitors endowed with picomolar inhibitory potency, active in cells and efficacious after oral administration in murine leukemia models. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2HPLC of Formula: 109384-19-2)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.HPLC of Formula: 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Misal Castro, Luis C.; Sultan, Ibrahim; Nishi, Kohei; Tsurugi, Hayato; Mashima, Kazushi published their research in Journal of Organic Chemistry in 2021. The article was titled 《Direct Synthesis of Indoles from Azoarenes and Ketones with Bis(neopentylglycolato)diboron Using 4,4′-Bipyridyl as an Organocatalyst》.Safety of 1-Methyl-4-piperidone The article contains the following contents:

Multifunctionalized indole derivatives were prepared by reducing azoarenes in the presence of ketones and bis(neopentylglycolato)diboron (B2nep2) with a catalytic amount of 4,4′-bipyridyl under neutral reaction conditions, where 4,4′-bipyridyl acted as an organocatalyst to activate the B-B bond of B2nep2 and form N,N’-diboryl-1,2-diarylhydrazines as a key intermediate. Further reaction of N,N’-diboryl-1,2-diarylhydrazines with ketones afforded N-vinyl-1,2-diarylhydrazines, which rearranged to the corresponding indoles via the Fischer indole mechanism. This organocatalytic system was applied to diverse alkyl cyclic ketones, dialkyl, and alkyl/aryl ketones, including heteroatoms. Me alkyl ketones gave the corresponding 2-methyl-3-substituted indoles in a regioselective manner. This protocol allowed us to expand the preparation of indoles having high compatibility with not only electron-donating and electron-withdrawing groups but also N- and O-protecting functional groups. In the part of experimental materials, we found many familiar compounds, such as 1-Methyl-4-piperidone(cas: 1445-73-4Safety of 1-Methyl-4-piperidone)

1-Methyl-4-piperidone(cas: 1445-73-4) is a member of piperidine. 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. Hence, continuous efforts have been made to develop convenient methods to prepare piperidine derivatives.Safety of 1-Methyl-4-piperidone

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2022,Wang, Chang; Qu, Lunjun; Chen, Xiaohong; Zhou, Qian; Yang, Yan; Zheng, Yan; Zheng, Xian; Gao, Liang; Hao, Jinqiu; Zhu, Lingyun; Pi, Bingxue; Yang, Chaolong published an article in Advanced Materials (Weinheim, Germany). The title of the article was 《Poly(arylene piperidine) Quaternary Ammonium Salts Promoting Stable Long-Lived Room-Temperature Phosphorescence in Aqueous Environment》.SDS of cas: 1445-73-4 The author mentioned the following in the article:

Room-temperature phosphorescence (RTP) materials have garnered considerable research attention owing to their excellent luminescence properties and potential application prospects in anti-counterfeiting, information storage, and optoelectronics. However, several RTP systems are extremely sensitive to humidity, and consequently, the realization of long-lived RTP in water remains a formidable challenge. Herein, a feasible and effective strategy is presented to achieve long-lived polymeric RTP systems, even in an aqueous environment, through doping of synthesized polymeric phosphor PBHDB into a poly(Me methacrylate) (PMMA) matrix. Compared to the precursor polymer PBN and organic mol. HDBP, a more rigid polymer microenvironment and electrostatic interaction are formed between the PMMA matrix and polymer PBHDB, which effectively reduce the nonradiative decay rate of triplet excitons and dramatically increase the phosphorescence intensity. Specifically, the phosphorescence lifetime of the PBHDB@PMMA film (1258.62 ms) is much longer than those of PBN@PMMA (674.20 ms) and HDBP@PMMA (1.06 ms). Most importantly, a bright-green afterglow can be observed after soaking the PBHDB@PMMA film in water for more than a month. The excellent water resistance and reversible response properties endow these systems with promising potential for dynamic information encryption even in water.1-Methyl-4-piperidone(cas: 1445-73-4SDS of cas: 1445-73-4) was used in this study.

1-Methyl-4-piperidone(cas: 1445-73-4) is a member of piperidine. Piperidine is ubiquitous structural motif widely occurred in diverse synthetically and naturally occurring bioactive molecules. Piperidines are an immensely important class of compounds medicinally: the piperidine ring is the most common heterocyclic subunit among FDA approved drugs.SDS of cas: 1445-73-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Related Products of 87120-72-7In 2021 ,《Identification of First-in-Class Inhibitors of Kallikrein-Related Peptidase 6 That Promote Oligodendrocyte Differentiation》 appeared in Journal of Medicinal Chemistry. The author of the article were Ait Amiri, Sabrina; Deboux, Cyrille; Soualmia, Feryel; Chaaya, Nancy; Louet, Maxime; Duplus, Eric; Betuing, Sandrine; Nait Oumesmar, Brahim; Masurier, Nicolas; El Amri, Chahrazade. The article conveys some information:

Multiple sclerosis (MS) is an autoimmune demyelinating disease of the central nervous system (CNS) that causes severe motor, sensory, and cognitive impairments. Kallikrein-related peptidase (KLK)6 is the most abundant serine protease secreted in the CNS, mainly by oligodendrocytes, the myelin-producing cells of the CNS, and KLK6 is assumed to be a robust biomarker of MS, since it is highly increased in the cerebrospinal fluid (CSF) of MS patients. Here, we report the design and biol. evaluation of KLK6′s low-mol.-weight inhibitors, para-aminobenzyl derivatives Interestingly, selected hit compounds were selective of the KLK6 proteolytic network encompassing KLK1 and plasmin that also participate in the development of MS physiopathol. Moreover, hits were found noncytotoxic on primary cultures of murine neurons and oligodendrocyte precursor cells (OPCs). Among them, two compounds (32 and 42) were shown to promote the differentiation of OPCs into mature oligodendrocytes in vitro constituting thus emerging leads for the development of regenerative therapies. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Related Products of 87120-72-7)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic amines have the nitrogen atom connected to an aromatic ring.Important amines include amino acids, biogenic amines, trimethylamine, and aniline. Inorganic derivatives of ammonia are also called amines, such as monochloramine (NClH2).Related Products of 87120-72-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Safety of 2-(Piperidin-4-yl)ethanolIn 2012 ,《Investigations of primary and secondary amine carbamate stability by 1H NMR spectroscopy for post combustion capture of carbon dioxide》 appeared in Journal of Chemical Thermodynamics. The author of the article were Fernandes, Debra; Conway, William; Burns, Robert; Lawrance, Geoffrey; Maeder, Marcel; Puxty, Graeme. The article conveys some information:

Carbamate formation is one of the major chem. reactions that can occur in solution in the capture of CO2 by amine-based solvents, and carbamate formation makes a significant enthalpy contribution to the absorption-desorption of CO2 that occurs in the absorber/stripper columns of the PCC process. Consequently, the formation of carbamates of selected series of primary and secondary amines over the temperature range (288 to 318) K has been investigated by equilibrium 1H NMR studies, and the stability constants (K 9) for the equilibrium:RNH2+HCO3-⇄K9RNHCOO-+H2Oare reported. van’t Hoff analyses have resulted in standard molar enthalpies, ΔHmo, and entropies, ΔSmo, of carbamate formation. A ΔHmo-ΔSmo plot generates a linear correlation for carbamate formation (providing a mean standard molar free energy, ΔGmo, for carbamate formation of about -7 kJ · mol-1), and this relationship helps provide a guide to the selection of an amine(s) solvent for CO2 capture, in terms of enthalpy considerations. A linear ΔHmo-ΔSmo plot also occurs for carbamate protonation. The formation of the carbamates has been correlated with systematic changes in composition and structure, and steric effects have been identified by comparing mol. geometries obtained using d. functional B3LYP/6-311++G(d,p) calculations Trends in steric effects have been identified in the series of compounds monoethanolamine (MEA), 1-amino-2-propanol, 2-amino-1-propanol (AP) and 2-amino-2-methyl-1-propanol (AMP). In the case of 2-piperidinemethanol, 2-piperidineethanol and 3-piperidinemethanol, strong intramol. hydrogen bonding is shown to be the likely cause for lack of carbamate formation, and in the ring systems of pyrrolidine, morpholine, piperidine and thiomorpholine trends in carbamate formation (as given by K 9) have been correlated with the internal ring angle at the amine nitrogen, as well as the planarity of the environment around the nitrogen atom. In the part of experimental materials, we found many familiar compounds, such as 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Safety of 2-(Piperidin-4-yl)ethanol)

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) have been used as an intermediate in the synthetic preparation of cellular-active allosteric inhibitors of FAKSafety of 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthetic Route of C6H11NOIn 2022 ,《Supported Anionic Gold Nanoparticle Catalysts Modified Using Highly Negatively Charged Multivacant Polyoxometalates》 was published in Angewandte Chemie, International Edition. The article was written by Xia, Kang; Yatabe, Takafumi; Yonesato, Kentaro; Yabe, Tomohiro; Kikkawa, Soichi; Yamazoe, Seiji; Nakata, Ayako; Yamaguchi, Kazuya; Suzuki, Kosuke. The article contains the following contents:

Although supported anionic gold nanoparticle catalysts have been theor. investigated for their efficacy in activating O2 in aerobic oxidation reactions, limited studies have been reported due to the difficulty of designing these catalysts. Herein, we developed a feasible method for preparing supported anionic gold nanoparticle catalysts using multivacant lacunary polyoxometalates with high neg. charges. We confirmed the strong and robust electronic interaction between gold nanoparticles and multivacant lacunary polyoxometalates, and the electronic states of the supported gold nanoparticle catalysts can be sequentially modulated. Particularly, the catalyst prepared using [SiW9O34]10- acted as an efficient reusable heterogeneous catalyst, showing superior catalytic performance for the oxidative dehydrogenation of piperidone derivatives to the corresponding enaminones and remarkably higher stability than supported gold nanoparticle catalysts without this modification. In the part of experimental materials, we found many familiar compounds, such as 1-Methyl-4-piperidone(cas: 1445-73-4Synthetic Route of C6H11NO)

1-Methyl-4-piperidone(cas: 1445-73-4) is a member of piperidine. Piperidine-containing compounds are also frequently employed in synthesis as ligands or auxiliaries. Accordingly, many efforts have been devoted to the development of novel methods for the synthesis of these compounds over the years.Synthetic Route of C6H11NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Recommanded Product: 622-26-4In 2013 ,《Investigation of temperature sensitivity behaviors of water soluble polyacrylamides》 was published in Journal of Applied Polymer Science. The article was written by Uguzdogan, Erdal; Denkbas, Emir Baki; Kabasakal, Osman Sermet. The article contains the following contents:

Temperature sensitive polymers with a lower critical solution temperature (LCST) are used in a variety of industries such as the pharmaceutical, cosmetic, food, and paint. These polymers are generally of the poly(N-alkylacrylamide) type, of which poly(N-isopropylacrylamide) (PNIPA) is the most commonly used. More novel poly(N-alkylacrylamide)s have also been the subject of much attention recently. In this study, N-alkylacrylamides containing different alkyl groups were synthesized by nucleophilic substitution reactions of various amines with acryloyl chloride. They were polymerized using the solution polymerization method, and the temperature sensitivities of the polymers were investigated. For this purpose, three monomers, N,N-diethylacrylamide, N-cyclopropylacrylamide, and 4-piperidineethanolacrylamide, were synthesized using diethylamine, cyclopropylamine, and 4-piperidineethanol, as the amines, resp. The obtained polymers, poly(N,N-diethylacrylamide) (PDEA), poly(N-cyclopropylacrylamide) (PCPA), and poly(4-piperidineethanolacrylamide) (PPEA), were found to be thermo-responsive, particularly PPEA is a potential novel material that can be utilized as an alternative to the common temperature sensitive polymers. The effects of several conditions on the LCST and the critical flocculation temperature (CFT) of the polymers were also investigated. © 2012 Wiley Periodicals, Inc. J. Appl. Polym. Sci., 2012.2-(Piperidin-4-yl)ethanol(cas: 622-26-4Recommanded Product: 622-26-4) was used in this study.

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) have been used as an intermediate in the synthetic preparation of cellular-active allosteric inhibitors of FAKRecommanded Product: 622-26-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Convenient, benign and scalable synthesis of 2- and 4-substituted benzylpiperidines》 was written by Agai, Bela; Proszenyak, Agnes; Tarkanyi, Gabor; Vida, Laszlo; Faigl, Ferenc. Electric Literature of C13H20ClNO And the article was included in European Journal of Organic Chemistry on August 27 ,2004. The article conveys some information:

A short, scalable and environmentally benign synthesis of 2- and 4-substituted benzylpiperidines, e.g. I, has been developed. The method is based on the temperature-programmed consecutive deoxygenation and heteroaromatic ring saturation of aryl(pyridin-2-yl)- and aryl(pyridin-4-yl)methanols and aryl(pyridin-4-yl)methanones in the presence of Pd/C catalyst. The crucial roles of the temperature, the acidity and the substrate structure in the change of selectivity have been demonstrated by isolation of several substituted aryl(piperidine)methanols. The carbinols and ketones were prepared from com. available pyridinecarbaldehydes or 4-cyanopyridine and substituted bromobenzenes via organometallic intermediates. The results came from multiple reactions, including the reaction of 4-(3-Methoxybenzyl)piperidine hydrochloride(cas: 149986-58-3Electric Literature of C13H20ClNO)

4-(3-Methoxybenzyl)piperidine hydrochloride(cas: 149986-58-3) belongs to piperidines. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions. Electric Literature of C13H20ClNO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Straightforward access to N-trifluoromethyl amides, carbamates, thiocarbamates and ureas》 was written by Scattolin, Thomas; Bouayad-Gervais, Samir; Schoenebeck, Franziska. HPLC of Formula: 87120-72-7This research focused ontrifluoromethyl amide carbamate thiocarbamate ureas. The article conveys some information:

Amides and related carbonyl derivatives are of central importance across the phys. and life sciences1,2. As a key biol. building block, the stability and conformation of amides affect the structures of peptides and proteins as well as their biol. function. In addition, amide-bond formation is one of the most frequently used chem. transformations3,4. Given their ubiquity, a technol. that is capable of modifying the fundamental properties of amides without compromising on stability may have considerable potential in pharmaceutical, agrochem. and materials science. In order to influence the phys. properties of organic mols.-such as solubility, lipophilicity, conformation, pKa and (metabolic) stability-fluorination approaches have been widely adopted5-7. Similarly, site-specific modification with isosteres and peptidomimetics8, or in particular by N-methylation9, has been used to improve the stability, phys. properties, bioactivities and cellular permeabilities of compounds However, the N-trifluoromethyl carbonyl motif-which combines both N-methylation and fluorination approaches-has not yet been explored, owing to a lack of efficient methodol. to synthesize it. Here the authors report a straightforward method to access N-trifluoromethyl analogs of amides and related carbonyl compounds The strategy relies on the operationally simple preparation of bench-stable carbamoyl fluoride building blocks, which can be readily diversified to the corresponding N-CF3 amides, carbamates, thiocarbamates and ureas. This method tolerates rich functionality and stereochem., and the authors present numerous examples of highly functionalized compounds-including analogs of widely used drugs, antibiotics, hormones and polymer units. The results came from multiple reactions, including the reaction of tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7HPLC of Formula: 87120-72-7)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic amines have the nitrogen atom connected to an aromatic ring.Important amines include amino acids, biogenic amines, trimethylamine, and aniline. Inorganic derivatives of ammonia are also called amines, such as monochloramine (NClH2).HPLC of Formula: 87120-72-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem