Category: piperidines

Direct Catalytic Decarboxylative Amination of Aryl Acetic Acids was written by Kong, Duanyang;Moon, Patrick J.;Bsharat, Odey;Lundgren, Rylan J.. And the article was included in Angewandte Chemie, International Edition in 2020.Related Products of 120014-30-4 This article mentions the following:

The decarboxylative coupling of a carboxylic acid with an amine nucleophile provides an alternative to the substitution of traditional organohalide coupling partners. Benzoic and alkynyl acids may be directly aminated by oxidative catalysis. In contrast, methods for intermol. alkyl carboxylic acid to amine conversion, including amidate rearrangements and photoredox-promoted approaches, require stoichiometric activation of the acid unit to generate isocyanate or radical intermediates. Reported here is a process for the direct chemoselective decarboxylative amination of electron-poor arylacetates by oxidative Cu catalysis. The reaction proceeds at (or near) room temperature, uses native carboxylic acid starting materials, and is compatible with protic, electrophilic, and other potentially complicating functionality. Mechanistic studies support a pathway in which ionic decarboxylation of the acid generates a benzylic nucleophile which is aminated in a Chan-Evans-Lam-type process. 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: 120014-30-4Related Products of 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.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 bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Related Products of 120014-30-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis of dicyanomethyl and nitro substituted p-polyphenyls and their salts was written by Zauhar, Joseph;Bandrauk, Andre D.;Truong, Kim D.;Michel, Andre. And the article was included in Synthesis in 1995.Safety of 4,4′-Bipiperidine dihydrochloride This article mentions the following:

A one-step, medium-scale synthesis of several novel dicyanomethyl and nitro substituted p-polyphenyls from 4,4′- or 4”-diiodo-p-polyphenyls and from 4-iodo-4′- or 4”-nitro-p-polyphenyls, resp., and sodium malononitrile using a palladium catalyst is reported. A number of organic cation salts of these extended 蟺-electron systems are likewise described. In the experiment, the researchers used many compounds, for example, 4,4′-Bipiperidine dihydrochloride (cas: 78619-84-8Safety of 4,4′-Bipiperidine dihydrochloride).

4,4′-Bipiperidine dihydrochloride (cas: 78619-84-8) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. 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.Safety of 4,4′-Bipiperidine dihydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Preparation of 3-(蠅-hydroxyalkyl)-substituted N-methylpiperdines and N-methyl-2-piperidones was written by Schneider, Woldemar;Moehrle, Hans;Wede, Ulrich;Kaemmerer, E.. And the article was included in Archiv der Pharmazie und Berichte der Deutschen Pharmazeutischen Gesellschaft in 1967.Computed Properties of C9H18ClNO2 This article mentions the following:

1 – Methyl – 3 – (hydroxymethyl)pyridinium iodide was converted to the chloride with AgCl and then hydrogenated on 5% Rh/C to give 80.5% 1-methyl-3-(hydroxymethyl)piperidine (I), b11 104掳, HCl salt m. 132-4掳, also obtained from the bromide, m. 90-2掳 (prepared from 3-C5H4NCH2OH and MeBr) by catalytic reduction Hydrogenation of 3-C5H4NCH2CH2OH.HCl on PtO2 at room temperature during 20 hrs. gave the corresponding piperidine-HCl salt (II), m. 139掳 (Me2CO), also obtained by LiAlH4 reduction of ethyl 3-piperidylacetate-HCl, m. 146掳, in tetrahydrofuran. Methylation of II with HCO2H/CH2O gave 80.8% 1-methyl-3-(hydroxyethyl) piperidine (III), b0.2 75掳, dinitrobenzoate m. 74掳. Treatment of 8.6 g. III with a hot solution of 38.4 g. Hg(OAc)2 and 44.7 g. EDTA in 250 cc. 1% AcOH on a steam-bath under N gave after 7.5 hrs. precipitation of 23.5 g. Hg and 21.2% 1-methyl-3-(hydroxyethyl)-2-piperidone (IIIb), b0.15 118-21掳, phenylcarbamate m. 95-7掳. Similarly obtained were: 1-methyl-3-(hydroxypropyl)piperidine-HCl (IV), m. 141-3掳, dehydrogenated to yield the corresponding piperidone (V), b1 130掳, ethyl 4-nitroazoxybenzoate m. 129-31掳 (Me2CO-cyclohexane). Dehydrogenation of I failed to give the ketone, which is in agreement with the postulated mechanism that a five (e.g. IIIa) or six-membered-ring intermediate is necessary for 2-piperidone formation. Ir data for the compounds are given. In the experiment, the researchers used many compounds, for example, Ethyl 2-(piperidin-3-yl)acetate hydrochloride (cas: 16780-05-5Computed Properties of C9H18ClNO2).

Ethyl 2-(piperidin-3-yl)acetate hydrochloride (cas: 16780-05-5) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. 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.Computed Properties of C9H18ClNO2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Preparation and quality control of compound cyproheptadine hydrochloride gel was written by He, Mingchao;Wang, Zhongshu. And the article was included in Zhongguo Yaoye in 2006.Application In Synthesis of 4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride This article mentions the following:

The gel contained carbomer-940 as the base, triethanolamine as pH adjuster and ethylparaben as preservative. The contents of cyproheptadine hydrochloride (Cph) and dexamethasone acetate (Dxm) in gel were determined by dual-wavelength spectrophotometry and HPLC resp. The gel exhibited fine consistency and moderate viscosity. The average content of Cph in the gel was 101.29% with an average recovery of 101.56% (RSD = 1.90%). The average content of Dxm in the gel was 99.20% with an average recovery of 99.44% (RSD = 2.46%). In the experiment, the researchers used many compounds, for example, 4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5Application In Synthesis of 4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride).

4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride (cas: 969-33-5) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Application In Synthesis of 4-(5H-Dibenzo[a,d][7]annulen-5-ylidene)-1-methylpiperidine hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Enhanced attention and impulsive action following NMDA receptor GluN2B-selective antagonist pretreatment was written by Higgins, Guy A.;Silenieks, Leo B.;MacMillan, Cam;Sevo, Julia;Zeeb, Fiona D.;Thevarkunnel, Sandy. And the article was included in Behavioural Brain Research in 2016.Recommanded Product: 1-((1S,2S)-1-Hydroxy-1-(4-hydroxyphenyl)propan-2-yl)-4-phenylpiperidin-4-ol This article mentions the following:

NMDA GluN2B (NR2B) subtype selective antagonists are currently in clin. development for a variety of indications, including major depression. We previously reported the selective NMDA GluN2B antagonists Ro 63-1908 and traxoprodil, increase premature responding in a 5-choice serial reaction time task (5-CSRTT) suggesting an effect on impulsive action. The present studies extend these investigations to a Go-NoGo and delay discounting task, and the 5-CSRTT under test conditions of both regular (5 s) and short (2-5 s) multiple ITI (Intertrial interval). Dizocilpine was included for comparison. Both Ro 63-1908 (0.1-1 mg/kg SC) and traxoprodil (0.3-3 mg/kg SC) increased premature and perseverative responses in both 5-CSRT tasks and improved attention when tested under a short ITI test condition. Ro 63-1908 but not traxoprodil increased motor impulsivity (false alarms) in a Go-NoGo task. Dizocilpine (0.01-0.06 mg/kg SC) affected both measures of motor impulsivity and marginally improved attention. In a delay discounting test of impulsive choice, both dizocilpine and Ro 63-1908 decreased impulsive choice (increased choice for the larger, delayed reward), while traxoprodil showed a similar trend. Motor stimulant effects were evident following Ro 63-1908, but not traxoprodil treatment – although no signs of motor stereotypy characteristic of dizocilpine (>0.1 mg/kg) were noted. The findings of both NMDA GluN2B antagonists affecting measures of impulsive action and compulsive behavior may underpin emerging evidence to suggest glutamate signaling through the NMDA GluN2B receptor plays an important role in behavioral flexibility. The profiles between Ro 63-1908 and traxoprodil were not identical, perhaps suggesting differences between members of this drug class. In the experiment, the researchers used many compounds, for example, 1-((1S,2S)-1-Hydroxy-1-(4-hydroxyphenyl)propan-2-yl)-4-phenylpiperidin-4-ol (cas: 134234-12-1Recommanded Product: 1-((1S,2S)-1-Hydroxy-1-(4-hydroxyphenyl)propan-2-yl)-4-phenylpiperidin-4-ol).

1-((1S,2S)-1-Hydroxy-1-(4-hydroxyphenyl)propan-2-yl)-4-phenylpiperidin-4-ol (cas: 134234-12-1) 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: 1-((1S,2S)-1-Hydroxy-1-(4-hydroxyphenyl)propan-2-yl)-4-phenylpiperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Design and synthesis of orally active benzamide derivatives as potent serotonin 4 receptor agonist was written by Sonda, Shuji;Kawahara, Toshio;Murozono, Takahiro;Sato, Noriko;Asano, Kiyoshi;Haga, Keiichiro. And the article was included in Bioorganic & Medicinal Chemistry in 2003.Related Products of 654084-41-0 This article mentions the following:

A series of 4-amino-5-chloro-2-methoxy-N-(piperidin-4-ylmethyl)benzamide derivatives bearing an aralkylamino, alkylamino, benzoyl or phenylsulfonyl group at its side chain part at the 1-position on the piperidine ring was synthesized. They were evaluated for serotonin 4 (5-HT₄) receptor agonist activity by testing their ability to contract the isolated guinea-pig ascending colon. 4-Amino-5-chloro-2-methoxy-N-[1-[5-(1-methylindol-3-ylcarbonylamino)pentyl]piperidin-4-ylmethyl]benzamide (1a, Y-34959) and its related compounds possessed favorable pharmacol. profiles for gastrointestinal motility. Unfortunately, the compound 1a showed low bioavailability when given orally presumably due to its poor intestinal absorption rate. Replacement of the 1-methylindol-3-yl carbonylamino moiety of 1a with an aralkylamino (or alkylamino) group did not improve the intestinal absorption rate. Replacement of the 1-methylindol-3-ylcarbonylamino moiety with a benzoyl or phenylsulfonyl group increased the intestinal absorption rate compared with 1a. These compounds revealed good pharmacol. profiles for gastrointestinal motility and were superior to 1a in oral bioavailability. In the experiment, the researchers used many compounds, for example, 4-Amino-5-chloro-2-methoxy-N-(piperidin-4-ylmethyl)benzamide hydrochloride (cas: 654084-41-0Related Products of 654084-41-0).

4-Amino-5-chloro-2-methoxy-N-(piperidin-4-ylmethyl)benzamide hydrochloride (cas: 654084-41-0) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. 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.Related Products of 654084-41-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Insights into urticaria in pediatric and adult populations and its management with fexofenadine hydrochloride was written by Ansotegui, Ignacio J.;Bernstein, Jonathan A.;Canonica, Giorgio W.;Gonzalez-Diaz, Sandra N.;Martin, Bryan L.;Morais-Almeida, Mario;Murrieta-Aguttes, Margarita;Sanchez Borges, Mario. And the article was included in Allergy, Asthma, & Clinical Immunology in 2022.Product Details of 153439-40-8 This article mentions the following:

The present narrative review provides a comprehensive update of the current knowledge on urticaria, both in adult and pediatric populations, and on the safety and efficacy of fexofenadine hydrochloride (HCl) as a treatment option. A literature search was conducted on Embase and Medline. Clin. studies published in English and published between 1999 and 2020 were selected. Although the exact pathogenesis of urticaria is not fully understood, multiple pathways of mast cell activation are discussed to explain the existence of phenotypically different clin. manifestations of urticaria. An overview of the worldwide prevalence of chronic urticaria, including disease burden and patient’s quality of life is provided. The impact of urticaria on patient’s life differs on the basis of whether its form is acute or chronic, but pharmacol. approaches are most often needed to control the disabling symptoms. A summary of the current management of urticaria recommended by different guidelines across countries (Global; European; American; Australian; Asian; Japanese) is presented. Non-sedating, second-generation H₁-antihistamines are the preferred choice of treatment across several guidelines worldwide. Herein, the efficacy and safety of fexofenadine HCl, a representative second-generation H₁-antihistamine approved for the treatment of urticaria, is discussed. The occurrence of urticaria manifestations in COVID-19 patients is also briefly presented. The burden of acute and chronic urticaria is high for patients. Second generation anti-histamines such as fexofenadine HCl can help managing the symptoms. 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: 153439-40-8Product Details of 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. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. 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.Product Details of 153439-40-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Chiral NMR discrimination of amines: analysis of secondary, tertiary, and prochiral amines using (18-crown-6)-2,3,11,12-tetracarboxylic acid was written by Lovely, Ann E.;Wenzel, Thomas J.. And the article was included in Chirality in 2008.Safety of Ethyl 1-methylpipecolinate This article mentions the following:

Enantiomeric discrimination is observed in the ¹H and ¹³C NMR spectra of secondary and tertiary amines in the presence of (-)-(18-crown-6)-2,3,11,12-tetracarboxylic acid (1). Nonequivalence of the resonances of prochiral nuclei in primary and secondary amines is also observed when they associated with 1. The amines are added in their neutral form and are protonated by the carboxylic acid groups of 1 to produce the corresponding ammonium and carboxylate ions. Secondary amines associate with 1 through two hydrogen bonds and an ion pair interaction. Tertiary amines can only form one hydrogen bond to accompany the ion pairing. Chiral discrimination in the ¹H and ¹³C NMR spectra of a series of aryl-containing secondary amines is of sufficient magnitude to determine enantiomeric purities. The discrimination in the spectra of tertiary amines with 1 is smaller, but ¹³C NMR spectra provided enough distinction for the determination of enantiomeric purity. In the experiment, the researchers used many compounds, for example, Ethyl 1-methylpipecolinate (cas: 30727-18-5Safety of Ethyl 1-methylpipecolinate).

Ethyl 1-methylpipecolinate (cas: 30727-18-5) 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.Safety of Ethyl 1-methylpipecolinate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Multiplexed holographic gratings recorded by 405 nm laser in polymer film containing spirooxazines was written by Fu, Shengcheng;Sun, Shiyu;Sang, Wenling;Sun, Bo;Zhang, Xintong;Liu, Yichun. And the article was included in Proceedings of SPIE in 2012.Related Products of 114747-45-4 This article mentions the following:

Multiple holog. gratings were recorded by 405 nm laser in the same location of spirooxazine doped polymer films using peristrophic multiplexing techniques. Diffraction efficiency of each grating was controlled almost uniform by adjusting recording time. It was found that the growth rate of the holog. grating recorded later was lower than that of the earlier one, resulting from the decreased population of spirooxazine mols. A kinetics description for the overlapped isomerization gratings agrees well with exptl. results. Due to the thermal stability of the isomerization grating, multiple interference fringes in the photochromic film were reserved and observed by Confocal Laser Scanning Microscope. In the experiment, the researchers used many compounds, for example, 1,3,3-Trimethyl-6′-(piperidin-1-yl)spiro[indoline-2,3′-naphtho[2,1-b][1,4]oxazine] (cas: 114747-45-4Related Products of 114747-45-4).

1,3,3-Trimethyl-6′-(piperidin-1-yl)spiro[indoline-2,3′-naphtho[2,1-b][1,4]oxazine] (cas: 114747-45-4) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. 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.Related Products of 114747-45-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Stereoselective Intermolecular Nitroaminoxylation of Terminal Aromatic Alkynes: Trapping Alkenyl Radicals by TEMPO was written by Yan, Hong;Rong, Guangwei;Liu, Defu;Zheng, Yang;Chen, Jie;Mao, Jincheng. And the article was included in Organic Letters in 2014.Electric Literature of C11H21N2O2 This article mentions the following:

The vinyl radical is one of the most unstable organic radicals. It is demonstrated that a nitro radical attacks phenylacetylene and makes the Ph ring deconjugated with a double bond so that the resulting vinyl radical may be stabilized by delocalization to the Ph ring’s 蟺 orbital and easily trapped by TEMPO. It is noteworthy that all desired products were obtained in moderate to good yields in an (E)-configuration. In the experiment, the researchers used many compounds, for example, 4-Acetamido-2,2,6,6-tetramethylpiperidine 1-oxyl (cas: 14691-89-5Electric Literature of C11H21N2O2).

4-Acetamido-2,2,6,6-tetramethylpiperidine 1-oxyl (cas: 14691-89-5) 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. 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.Electric Literature of C11H21N2O2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem