Category: piperidines

From Zn(C₆F₅)₂ to ZnEt₂-based Lewis Pairs: Significantly Improved Catalytic Activity and Monomer Adaptability for the Ring-opening Polymerization of Lactones was written by Wang, Bin;Wei, Yuan;Li, Zong-Jun;Pan, Li;Li, Yue-Sheng. And the article was included in ChemCatChem in 2018.HPLC of Formula: 79-55-0 This article mentions the following:

In this contribution, the structure-reactivity relationships of ZnR₂/DMAP (R=C₆F₅, C₆H₅ and C₂H₅) Lewis pairs in ring-opening polymerization (ROP) of lactones were investigated by crystallog. anal., d. functional theory (DFT) calculations and kinetic studies. With decrease of ZnR₂ Lewis acidity, the interaction between ZnR₂ and DMAP weakens and the dissociation of ZnR₂路2DMAP Lewis adducts become easier, which facilitates the activation of cyclic ester monomers. Thus, the ZnEt₂/DMAP Lewis pair, bearing weakest interaction between Lewis acid and Lewis base, exhibits high catalytic activity and broad monomer adaptability. ZnEt₂路2DMAP can convert lactide (LA) rapidly into polylactide (PLA) even at room temperature Furthermore, a wide range of cyclic esters can also be polymerized using this dual catalyst, from small lactones such as 尾-butyrolactone (尾-BL), 未-valerolactone (未-VL) and 蔚-caprolactone (蔚-CL) to the strainless macrolactone. The optimal reaction pathway, key species and active species in the ZnEt₂路2DMAP catalytic ROP of LA were figured out by DFT calculations The results clearly indicated that a DMAP-LA exchange was necessary for activation of monomer, and the single mol. initiation is preferred. Meanwhile, the cyclic active species is more stable than the linear analogs, in which DMAP and ZnEt₂ bond with each polymer chain end resp. and ZnEt₂ interact with DMAP. The DFT calculation gives an account for the formation of the cyclic polyester in the ROP of LA by ZnR₂-based Lewis pairs. In the experiment, the researchers used many compounds, for example, 1,2,2,6,6-Pentamethylpiperidine (cas: 79-55-0HPLC of Formula: 79-55-0).

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. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.HPLC of Formula: 79-55-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Effects of methimepip and JNJ-5207852 in Wistar rats exposed to an open-field with and without object and in Balb/c mice exposed to a radial-arm maze was written by Abuhamdah, Rushdie M. A.;van Rensburg, Ruan;Lethbridge, Natasha L.;Ennaceur, Abdel;Chazot, Paul L.. And the article was included in Frontiers in Systems Neuroscience in 2012.Recommanded Product: 1-(4-(3-(Piperidin-1-yl)propoxy)benzyl)piperidine This article mentions the following:

The role of the histamine H₃ receptor (H₃R) in anxiety is controversial, due to limitations in drug selectivity and limited validity of behavioral tests used in previous studies. In the present report, we describe two experiments In the first one, Wistar rats were treated with an H₃R agonist (methimepip) and exposed to an open-field. In the second one, Balb/c mice were treated with H₃R agonist (methimepip) or antagonist (JNJ-5207852) and exposed to an open space 3D maze which is a modified version of the radial-arm maze. C57BL/6J saline treated mice were included for comparisons. When exposed to an empty open field, Wistar rats spent more time in the outer area and made very low number of brief crossings in the central area. However, when an object occupied the central area, rats crossed frequently into and spent a long time in the central area. Administration of a range of different doses of methimepip (selective H₃R agonist) reduced the entries into the central area with a novel object, indicating enhanced avoidance response. In the 3D maze, both Balb/c and C57BL/6J saline-treated mice crossed frequently onto the bridges that radiate from the central platform but only C57BL/6J mice crossed onto the arms which extend the bridges. This suggests that Balb/c mice are more anxious than C57BL/6J mice. Neither methimepip nor JNJ-5207852 (selective H₃R antagonist/inverse agonist) induced entry into the arms of the maze, indicative of lack of anxiolytic effects. In the experiment, the researchers used many compounds, for example, 1-(4-(3-(Piperidin-1-yl)propoxy)benzyl)piperidine (cas: 398473-34-2Recommanded Product: 1-(4-(3-(Piperidin-1-yl)propoxy)benzyl)piperidine).

1-(4-(3-(Piperidin-1-yl)propoxy)benzyl)piperidine (cas: 398473-34-2) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. 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.Recommanded Product: 1-(4-(3-(Piperidin-1-yl)propoxy)benzyl)piperidine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Rational Design of Original Fused-Cycle Selective Inhibitors of Tryptophan 2,3-Dioxygenase was written by Kozlova, Arina;Thabault, Leopold;Liberelle, Maxime;Klaessens, Simon;Prevost, Julien R. C.;Mathieu, Caroline;Pilotte, Luc;Stroobant, Vincent;Van den Eynde, Benoit;Frederick, Raphael. And the article was included in Journal of Medicinal Chemistry in 2021.HPLC of Formula: 144222-22-0 This article mentions the following:

Tryptophan 2,3-dioxygenase (TDO2) is a heme-containing enzyme constitutively expressed at high concentrations in the liver and responsible for L-tryptophan (L-Trp) homeostasis. Expression of TDO2 in cancer cells results in the inhibition of immune-mediated tumor rejection due to an enhancement of L-Trp catabolism via the kynurenine pathway. In the study herein, we disclose a new 6-(1H-indol-3-yl)-benzotriazole scaffold of TDO2 inhibitors developed through rational design, starting from existing inhibitors. Rigidification of the initial scaffold led to the synthesis of stable compounds displaying a nanomolar cellular potency and a better understanding of the structural modulations that can be accommodated inside the active site of hTDO2. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0HPLC of Formula: 144222-22-0).

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. 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.HPLC of Formula: 144222-22-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Design, Synthesis, and Biological Evaluation of Orally Bioavailable CHK1 Inhibitors Active against Acute Myeloid Leukemia was written by Jin, Tingting;Wang, Peipei;Long, Xiubing;Jiang, Kailong;Song, Pinrao;Wu, Wenbiao;Xu, Gaoya;Zhou, Yubo;Li, Jia;Liu, Tao. And the article was included in ChemMedChem in 2021.Recommanded Product: 144222-22-0 This article mentions the following:

Checkpoint kinase 1 (CHK1) is a central component in DNA damage response and has emerged as a target for antitumor therapeutics. Herein, we describe the design, synthesis, and biol. evaluation of a novel series of potent diaminopyrimidine CHK1 inhibitors. The compounds exhibited moderate to potent CHK1 inhibition and could suppress the proliferation of malignant hematol. cell lines. The optimized compound 13 had a CHK1 IC50 value of 7.73卤0.74 nM, and MV-4-11 cells were sensitive to it (IC50=0.035卤0.007渭M). Furthermore, compound 13 was metabolically stable in mouse liver microsomes in vitro and displayed moderate oral bioavailability in vivo. Moreover, treatment of MV-4-11 cells with compound 13 for 2 h led to robust inhibition of CHK1 autophosphorylation on serine 296. Based on these biochem. results, we consider compound 13 to be a promising CHK1 inhibitor and potential anticancer therapeutic agent. 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 saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Recommanded Product: 144222-22-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

UV spectrophotometric derivative methods for estimation of fexofenadine hydrochloride in bulk drug and pharmaceutical dosage form was written by Rele, Rajan V.. And the article was included in Journal of Chemical and Pharmaceutical Research in 2016.HPLC of Formula: 153439-40-8 This article mentions the following:

Simple and precise UV spectrophotometric methods by second and third order derivative have been developed and validated for the estimation of fexofenadine hydrochloride in bulk and its tablet formulation. The standard and sample solutions of fexofenadine hydrochloride were prepared in 0.1 N Hydrochloric acid. Fexofenadine hydrochloride was estimated at 215 nm for the second order derivative and 233.7 nm for third order derivative resp. Beer’s law was obeyed in the concentration range of 1 to 14 渭g / ml with coefficient of correlation values were 0.9992 for second order derivative method and 0.9997 for third order derivative method resp. These methods were tested and validated for various parameters according to ICH guidelines. The precision expressed as relative standard deviation were of 0.8908 % and 1.152% for the above two methods resp. The proposed methods were successfully applied for the determination of fexofenadine hydrochloride in pharmaceutical formulation. Results of the anal. were validated statistically and were found to be satisfactory. The proposed methods are simple, easy to apply, low-cost and require relatively inexpensive instruments. 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: 153439-40-8HPLC of Formula: 153439-40-8).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid hydrochloride (cas: 153439-40-8) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. 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.HPLC of Formula: 153439-40-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

CO₂ absorption performance in advanced water-lean diamine solvents was written by Xu, Yanjie;Wang, Tao;Yang, Qi;Yu, Hai;Fang, Mengxiang;Puxty, Graeme. And the article was included in Chemical Engineering Journal (Amsterdam, Netherlands) in 2021.SDS of cas: 41838-46-4 This article mentions the following:

In an effort to reduce energy penalties, a range of advanced water-lean solutions blended from one of 8 diamines, an organic solvent diluent and water, were screened. The diamines N,N-dimethyl-1,3-propanediamine and N,N-dimethyl-1,2-ethanediamine with one primary and one tertiary amino group remain homogenous during CO₂ uptake with the addition of cosolvents (1-methyl-2-pyrrolidinone or sulfolane) and are further investigated for absorption and desorption performance compared with their corresponding aqueous solutions Water-lean solutions with different water concentrations are tested to explain the impact of water content on the solution performance. Phys. properties such as d. and viscosity are also measured for a versatile evaluation. The results show that diamine water-lean solutions obtain low viscosity, preferable cyclic capacities and rapid absorption and desorption rates. ENH-5% H₂O (mass ratio DMEDA: NMP: H₂O = 3:6.5:0.5) shows the most competitive advantages with comparable viscosity (1.49 mPa鈥 at 313 K) to aqueous MEA-H₂O and a 140% improvement in cyclic capacity. Four-fold higher desorption rate is gained ESH-5%H₂O (mass ratio DMEDA: SFL: H₂O = 3:6.5:0.5) compared with MEA-H₂O. Considerable reduction in energy penalties is expected to be achieved in diamine water-lean solutions In addition, the equilibrium solubility of diamine water-lean solutions also shows potential for industrial application due to their sensitivity to CO₂ partial pressure in contrast with aqueous solutions In the experiment, the researchers used many compounds, for example, 4-Amino-1-methylpiperidine (cas: 41838-46-4SDS of cas: 41838-46-4).

4-Amino-1-methylpiperidine (cas: 41838-46-4) 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. 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.SDS of cas: 41838-46-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis of Donepezil Hydrochloride via Chemoselective Hydrogenation was written by Rawat, Ajay Singh;Pande, Sachin;Bhatt, Nilay;Kharatkar, Raju;Belwal, Chandrakant;Vardhan, Anand. And the article was included in Organic Process Research & Development in 2013.Recommanded Product: 120014-30-4 This article mentions the following:

A simple and highly chemoselective and cost-effective process for the synthesis of Donepezil 1 has been developed for com. production In the process, the exocyclic double bond is mainly targeted for catalytic hydrogenation in the presence of an N-benzyl group using sulfur, nitrogen, and phosphorous catalyst modifiers. In some cases, catalytic hydrogenation with Pd on charcoal also produced an undesired side product along with the main product due to over reduction Removal of these impurities by crystallization, column chromatog., or other means of purification makes the process tedious and lengthy, and sometimes it is difficult to achieve the impurity limit as per International Conference on Harmonisation (ICH) guidelines for active pharmaceutical ingredients. In the present investigation we report the synthesis of Donepezil 1 in pure form wherein the debenzyl impurity is within the acceptable limits. 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: 120014-30-4Recommanded Product: 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.Recommanded Product: 120014-30-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Ionic liquids as stationary phase solvents for methylated cyclodextrins in gas chromatography was written by Berthod, A.;He, L.;Armstrong, D. W.. And the article was included in Chromatographia in 2001.Product Details of 1722-95-8 This article mentions the following:

Room temperature ionic liquids (RTIL) are molten salts with m.ps. well below room temperature 1-Butyl-3-methylimidazolium chloride is a typical example of such RTIL. It was used as a solvent to dissolve permethylated-尾-cyclodextrin (BPM) and dimethylated-尾-cyclodextrin (BDM) to prepare stationary phases for capillary columns in gas chromatog. for chiral separation The RTIL containing columns were compared to com. columns containing the same chiral selectors. A set of 64 chiral compounds separated by the com. BPM column was tested on the RTIL BPM column. Only 21 were enantioresolved. Similarly, a set of 80 compounds separated by the com. BDM column was passed on the RTIL BDM column with only 16 pos. separations Probably the imidazolium ion pair could make an inclusion complex with the cyclodextrin cavity, blocking it for chiral recognition. All the chiral compounds recognized by the RTIL columns had their asym. carbon that was part of a ring structure. The retention factors of the derivatized solutes were lower on the RTIL columns than those obtained on the com. equivalent column. The peak efficiencies obtained with the RTIL capillary were significantly higher than that obtained with the com. column. These observations may contribute to the knowledge of the mechanism of cyclodextrin-based GC enantioselective separations In the experiment, the researchers used many compounds, for example, (R)-2-Methylpiperidine (cas: 1722-95-8Product Details of 1722-95-8).

(R)-2-Methylpiperidine (cas: 1722-95-8) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Product Details of 1722-95-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

An adsorption study on STA-16(Co) was written by Patzschke, Christin;Marshall, Marc;Chaffee, Alan L.. And the article was included in Microporous and Mesoporous Materials in 2016.Recommanded Product: 4,4′-Bipiperidine dihydrochloride This article mentions the following:

Adsorption is considered a promising method for carbon capture. CO₂ adsorbents take a variety of forms, but one approach is the use of metal-organic frameworks (MOFs). In this study, the potential of STA-16(Co) to selectively adsorb and sep. CO₂ is considered. Isotherms for CO₂ and N₂ were measured from 0 to 25 bar at temperatures between 25 and 105 掳C to evaluate the potential application in high pressure separation processes. Low pressure CO₂ pseudo-isotherms were measured from 0 to 0.5 bar at temperatures between 25 and 105 掳C, together with dry and wet cycling experiments, to determine the applicability of STA-16(Co) in a vacuum swing adsorption (VSA) process. The presence of 1% H₂O vapor during ten cycle experiments resulted in a decrease in CO₂ working capacity obtained under dry cyclic conditions of 鈭?6% due to the high H₂O uptake. In contrast to the majority of MOFs, STA-16(Co) exhibited a good H₂O stability and maintained its CO₂ adsorption capacity after adsorption/desorption of H₂O vapor at 30 and 60% RH at 25 掳C. However the treatment at 90% RH resulted in a small decrease in CO₂ adsorption capacity, apparently due to the formation of a different crystal structure. In the experiment, the researchers used many compounds, for example, 4,4′-Bipiperidine dihydrochloride (cas: 78619-84-8Recommanded Product: 4,4′-Bipiperidine dihydrochloride).

4,4′-Bipiperidine dihydrochloride (cas: 78619-84-8) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Recommanded Product: 4,4′-Bipiperidine dihydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Versatile strategy for fabrication of polypropylene nanocomposites with inorganic network structures based on catalyzed in-situ sol-gel reaction during melt mixing was written by Kaneko, Kei;Yadav, Nitin;Takeuchi, Kengo;Maira, Bulbul;Terano, Minoru;Taniike, Toshiaki. And the article was included in Composites Science and Technology in 2014.Electric Literature of C30H56N2O4 This article mentions the following:

A versatile strategy based on a catalyzed in-situ sol-gel reaction in melt mixing was presented for the fabrication of polypropylene (PP) nanocomposites that equip inorganic network structures. PP nanocomposites with TiO₂ network structures were obtained by melt mixing PP powder which was preliminarily impregnated with titanium alkoxide and a catalytic component. The addition of catalytic components, especially hindered amine stabilizer, was found to be effective not only for the acceleration of the in-situ sol-gel reaction but also for improved dispersion of formed inorganic nanoparticles. The obtained PP/TiO₂ nanocomposites exhibited the disappearance of the terminal flow at ca. 3 wt% of the TiO₂ content, indicative of the network formation. Moreover, the PP/TiO₂ nanocomposite films exhibited distinct optical properties: not only high transparency for visible lights due to the excellent dispersion of the made nanoparticles but also absorption of UV lights, where absorption edges were tunable through a quantum effect for nanosized particles. In the experiment, the researchers used many compounds, for example, Bis(1,2,2,6,6-pentamethylpiperidin-4-yl) decanedioate (cas: 41556-26-7Electric Literature of C30H56N2O4).

Bis(1,2,2,6,6-pentamethylpiperidin-4-yl) decanedioate (cas: 41556-26-7) 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. 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.Electric Literature of C30H56N2O4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem