Month: October 2022

Name: 2-(Piperidin-4-yl)ethanolIn 2020 ,《Discovery of 2-(4-(2-fluoroethoxy)piperidin-1-yl)-9-methyl-9H-pyrrolo[2,3-b:4,5-c’]dipyridine ([18F]PI-2014) as PET tracer for the detection of pathological aggregated tau in Alzheimer’s disease and other tauopathies》 appeared in European Journal of Medicinal Chemistry. The author of the article were Gabellieri, Emanuele; Capotosti, Francesca; Molette, Jerome; Sreenivasachary, Nampally; Mueller, Andre; Berndt, Mathias; Schieferstein, Hanno; Juergens, Tanja; Varisco, Yvan; Oden, Felix; Schmitt-Willich, Heribert; Hickman, David; Dinkelborg, Ludger; Stephens, Andrew; Pfeifer, Andrea; Kroth, Heiko. The article conveys some information:

The compound screening was initiated with a direct staining assay to identify compounds binding to Tau aggregates and not Abeta plaques using human brain sections derived from late stage Alzheimer’s disease donors. The binding of Tau aggregate selective compounds was then quant. assessed with human brain derived paired helical filaments utilizing the label-free Back Scattering Interferometry assay. In vivo biodistribution experiments of selected fluorine-18 labeled compounds were performed in mice to assess brain uptake, brain washout, and defluorination. Compound 11 emerged as the most promising candidate, displaying high in vitro binding affinity and selectivity to neurofibrillary tangles. Fluorine-18 labeled compound 11 showed high brain uptake and rapid washout from the mouse brain with no observed bone uptake. Furthermore, compound 11 was able to detect Tau aggregates in tauopathy brain sections from corticobasal degeneration, progressive supranuclear palsy, and Pick’s disease donors. Thus, 2-(4-(2-fluoroethoxy)piperidin-1-yl)-9-methyl-9H-pyrrolo[2,3-b:4,5-c’]dipyridine (PI-2014, compound 11) was selected for characterization in a first-in-human study. In addition to this study using 2-(Piperidin-4-yl)ethanol, there are many other studies that have used 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Name: 2-(Piperidin-4-yl)ethanol) 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 FAKName: 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Piperidine-4-carboxamides target DNA gyrase in Mycobacterium abscessus》 was written by Negatu, Dereje Abate; Beuchel, Andreas; Madani, Abdeldjalil; Alvarez, Nadine; Chen, Chao; Aragaw, Wassihun Wedajo; Zimmerman, Matthew D.; Laleu, Benoit; Gengenbacher, Martin; Dartois, Veronique; Imming, Peter; Dicka, Thomas. SDS of cas: 39546-32-2 And the article was included in Antimicrobial Agents and Chemotherapy on August 31 ,2021. The article conveys some information:

New, more-effective drugs for the treatment of lung disease caused by nontuberculous mycobacteria (NTM) are needed. Among NTM opportunistic pathogens, Mycobacterium abscessus is the most difficult to cure and intrinsically multidrug resistant. In a whole-cell screen of a compound collection active against Mycobacterium tuberculosis, we previously identified the piperidine-4-carboxamide (P4C) MMV688844 (844) as a hit against M. abscessus. Here, we identified a more potent analog of 844 and showed that both the parent and improved analog retain activity against strains representing all three subspecies of the M. abscessus complex. Furthermore, P4Cs showed bactericidal and antibiofilm activity. Spontaneous resistance against the P4Cs emerged at a frequency of 10-8/CFU and mapped to gyrA and gyrB encoding the subunits of DNA gyrase. Biochem. studies with recombinant M. abscessus DNA gyrase showed that P4Cs inhibit the wild-type enzyme but not the P4C-resistant mutant. P4C-resistant strains showed limited cross-resistance to the fluoroquinolone moxifloxacin, which is in clin. use for the treatment of macrolide-resistant M. abscessus disease, and no cross-resistance to the benzimidazole SPR719, a novel DNA gyrase inhibitor in clin. development for the treatment of mycobacterial diseases. Analyses of P4Cs in recA promoter-based DNA damage reporter strains showed induction of recA promoter activity in the wild type but not in the P4C-resistant mutant background. This indicates that P4Cs, similar to fluoroquinolones, cause DNA gyrase-mediated DNA damage. Together, our results show that P4Cs present a novel class of mycobacterial DNA gyrase inhibitors with attractive antimicrobial activities against the M. abscessus complex. After reading the article, we found that the author used Piperidine-4-carboxamide(cas: 39546-32-2SDS of cas: 39546-32-2)

Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. Amines characteristically form salts with acids; a hydrogen ion, H+, adds to the nitrogen. With the strong mineral acids (e.g., H2SO4, HNO3, and HCl), the reaction is vigorous. Salt formation is instantly reversed by strong bases such as NaOH. Neutral electrophiles (compounds attracted to regions of negative charge) also react with amines; alkyl halides (R′X) and analogous alkylating agents are important examples of electrophilic reagents.SDS of cas: 39546-32-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Synthesis, characterization and antimicrobial activity of piperidine derivatives》 was published in Journal of the Chemical Society of Pakistan in 2019. These research results belong to Zafar, Shaista; Akhtar, Shamim; Ali, Syed Imran; Mushtaq, Nausheen; Naeem, Sabahat; Ali, Mohsin. Product Details of 39546-32-2 The article mentions the following:

Synthesis of various piperidine derivatives having important biol. and pharmacol. potentials has been discussed in the past. In present study we reported the synthesis of benzoyl and sulfonyl derivatives by taking Piperidine-4-carboxamide as principal mol. These compounds were characterized by various spectroscopic techniques such as NMR, FTIR and Mass spectrometry. Elemental composition was explored using CHN analyzer. Antimicrobial activity study of the synthesized compounds was performed using disk diffusion method. Dissociation constant (pKa) of the synthesized compounds were determined by potentiometric titration method. In addition The findings of the study predicted good absorption of these newly synthesized compounds Besides, compound III showed good antifungal activity which can be helpful in pharmacokinetics and pharmacodynamics approaches of antibiotics. In the experiment, the researchers used Piperidine-4-carboxamide(cas: 39546-32-2Product Details of 39546-32-2)

Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. Amines have a free lone pair with which they can coordinate to metal centers. Amine–metal bonds are weaker because amines are incapable of backbonding, but they are still important for sensing applications.While stronger than hydrogen bonds, amine–metal bonds are still weaker than both covalent and ionic bonds.Product Details of 39546-32-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Product Details of 194726-40-4On May 10, 2018 ,《Strategic Approaches to Overcome Resistance against Gram-Negative Pathogens Using β-Lactamase Inhibitors and β-Lactam Enhancers: Activity of Three Novel Diazabicyclooctanes WCK 5153, Zidebactam (WCK 5107), and WCK 4234》 appeared in Journal of Medicinal Chemistry. The author of the article were Papp-Wallace, Krisztina M.; Nguyen, Nhu Q.; Jacobs, Michael R.; Bethel, Christopher R.; Barnes, Melissa D.; Kumar, Vijay; Bajaksouzian, Saralee; Rudin, Susan D.; Rather, Philip N.; Bhavsar, Satish; Ravikumar, Tadiparthi; Deshpande, Prasad K.; Patil, Vijay; Yeole, Ravindra; Bhagwat, Sachin S.; Patel, Mahesh V.; van den Akker, Focco; Bonomo, Robert A.. The article conveys some information:

Limited treatment options exist to combat infections caused by multidrug-resistant (MDR) Gram-neg. bacteria possessing broad-spectrum β-lactamases. The design of novel β-lactamase inhibitors is of paramount importance. Here, three novel diazabicyclooctanes (DBOs), WCK 5153, zidebactam (WCK 5107), and WCK 4234 (compounds 1-3, resp.), were synthesized and biochem. characterized against clin. important bacteria. Compound 3 inhibited class A, C, and D β-lactamases with unprecedented k2/K values against OXA carbapenemases. Compounds 1 and 2 acylated class A and C β-lactamses rapidly but not the tested OXAs. Compounds 1-3 formed highly stable acyl-complexes as demonstrated by mass spectrometry. Crystallog. revealed that 1-3 complexed with KPC-2 adopted a “”chair conformation”” with the sulfate occupying the carboxylate binding region. The cefepime-2 and meropenem-3 combinations were effective in murine peritonitis and neutropenic lung infection models caused by MDR Acinetobacter baumannii. Compounds 1-3 are novel β-lactamase inhibitors that demonstate potent cross-class inhibition, and clin. studies targeting MDR infections are warranted. In the part of experimental materials, we found many familiar compounds, such as (R)-1-tert-Butyl 3-ethyl piperidine-1,3-dicarboxylate(cas: 194726-40-4Product Details of 194726-40-4)

(R)-1-tert-Butyl 3-ethyl piperidine-1,3-dicarboxylate(cas: 194726-40-4) 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.Product Details of 194726-40-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Category: piperidinesOn September 30, 2018 ,《Diastereoselective synthesis of 2-vinylpyrrolidines and 2-vinylpiperidines by the palladium-catalysed cyclization of amino-allylic carbonates containing a chiral protecting group》 was published in ARKIVOC (Gainesville, FL, United States). The article was written by Olszewska, Beata; Jablonska, Aleksandra; Zawisza, Anna. The article contains the following contents:

An efficient diastereoselective synthesis of pyrrolidine- and piperidine-type N-heterocycles was reported, by the intramol. Pd(0)-catalyzed cyclization of amino carbonates containing chiral protecting group. The use of chiral auxiliary in the cyclization gave the corresponding heterocyclic derivatives in excellent yields and with good dr values. In the experiment, the researchers used many compounds, for example, (S)-2-Ethylpiperidine hydrochloride(cas: 558479-16-6Category: piperidines)

(S)-2-Ethylpiperidine hydrochloride(cas: 558479-16-6) 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

Vastyl, Michal; Jankovska, Zuzana; Cruz, Gerardo Juan Francisco; Matejova, Lenka published an article on February 28 ,2022. The article was titled 《A case study on microwave pyrolysis of waste tyres and cocoa pod husk; effect on quantity and quality of utilizable products》, and you may find the article in Journal of Environmental Chemical Engineering.Quality Control of Triacetonamine The information in the text is summarized as follows:

Disposal of huge amounts of diverse wastes for reduced costs accompanied with gaining of energy and valuable chems. is an eager topic in waste-to-energy and fuel business. Microwave pyrolysis is a thermochem. route providing such benefits. Waste scrap tyres (ST) and cocoa pod husk (CPH) as polymer and biomass representatives were pyrolyzed in microwave reactor at 440 W power for 30 min. Quantity and quality of pyrolysis products (gas, oil, and carbon black) were investigated. It was revealed, while set microwave pyrolysis conditions are sufficient for maximum decomposition of ST to pyrolysis products, it is necessary to optimize them for CPH. The gas produced by microwave pyrolysis of ST contains more H2 and CH4 than from conventional pyrolysis, thus, microwave pyrolysis is an effective tool for production of a fuel gas. The oil obtained by ST microwave pyrolysis is a complex mixture of mostly nonpolar aromatic compounds (toluene, benzene, limonene, styrene, o-xylene), while the oil obtained by CPH microwave pyrolysis contains mainly p-cresol, phenol and its derivatives The ST-derived carbon black shows a well-established large-volume mesoporous-macroporous structure. The CPH-derived carbon black is a low-volume macroporous material with very well-developed microporosity. A higher gross calorific value of microwave ST-derived carbon black in comparison to conventionally prepared one is caused by its higher graphitization rate. Since the surface of ST-derived carbon black is more polar than CPH-derived one and with respect to chem. purity, it could be more suitable adsorbent for polar volatile organic compounds from gaseous emissions. It is necessary to develop a microporosity in ST-derived carbon black. In addition to this study using Triacetonamine, there are many other studies that have used Triacetonamine(cas: 826-36-8Quality Control of Triacetonamine) was used in this study.

Triacetonamine(cas: 826-36-8) 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.Quality Control of Triacetonamine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2022,Yen-Pon, Expedite; Li, Longbo; Levitre, Guillaume; Majhi, Jadab; McClain, Edward J.; Voight, Eric A.; Crane, Erika A.; Molander, Gary A. published an article in Journal of the American Chemical Society. The title of the article was 《On-DNA Hydroalkylation to Introduce Diverse Bicyclo[1.1.1]pentanes and Abundant Alkyls via Halogen Atom Transfer》.Name: tert-Butyl 4-hydroxypiperidine-1-carboxylate The author mentioned the following in the article:

A Giese addition to install highly functionalized bicyclo[1.1.1]pentanes (BCPs) using tricyclo[1.1.1.01,3]pentane (TCP) as a radical linchpin, as well as other diverse alkyl groups, on-DNA from the corresponding organohalides as non-stabilized radical precursors was reported. Telescoped procedures allow extension of the substrate pool by at least an order of magnitude to ubiquitous alcs. and carboxylic acids, allowing us to “”upcycle”” these abundant feedstocks to afford non-traditional libraries with different physicochem. properties for the small-mol. products (i.e., non-peptide libraries with acids). This approach is amenable to library production, as a DNA damage assessment revealed good PCR amplifiability and only 6% mutated sequences for a full-length DNA tag. The results came from multiple reactions, including the reaction of tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Name: tert-Butyl 4-hydroxypiperidine-1-carboxylate)

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.Name: tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Quality Control of 1-(Piperidin-4-yl)-1H-indoleOn June 2, 2003, Faul, Margaret M.; Gillig, James R.; Jirousek, Michael R.; Ballas, Lawrence M.; Schotten, Theo; Kahl, Astrid; Mohr, Michael published an article in Bioorganic & Medicinal Chemistry Letters. The article was 《Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCβ》. The article mentions the following:

The synthesis and structure-activity relationship (SAR) trends of a new class of N-(azacycloalkyl)bisindolylmaleimides, e.g. I (R1 = CH2-pyridyl, R2 = Me, n = 2), acyclic derivatives of staurosporine, is described. I exhibits an IC50 of 40-50 nM against the human PKCβ1 and PKCβ2 isoenzymes and selectively inhibits the PKCβ isoenzymes in comparison to other PKC isoenzymes (α, γ, δ, ε, λ, and η). The series is also kinase selective for PKC in comparison to other ATP-dependent kinases. A comparison of the protein kinase C (PKC) isoenzyme and kinase activity of the series is made to the kinase inhibitor staurosporine. In the experiment, the researchers used 1-(Piperidin-4-yl)-1H-indole(cas: 118511-81-2Quality Control of 1-(Piperidin-4-yl)-1H-indole)

1-(Piperidin-4-yl)-1H-indole(cas: 118511-81-2) belongs to piperidines. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions. Quality Control of 1-(Piperidin-4-yl)-1H-indole

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthetic Route of C9H17NOOn March 24, 2020, Tanaka, Susumu; Enoki, Toshiaki; Imoto, Hiroaki; Ooyama, Yousuke; Ohshita, Joji; Kato, Takuji; Naka, Kensuke published an article in Macromolecules (Washington, DC, United States). The article was 《Highly Efficient Singlet Oxygen Generation and High Oxidation Resistance Enhanced by Arsole-Polymer-Based Photosensitizer: Application as a Recyclable Photooxidation Catalyst》. The article mentions the following:

Photosensitizers have attracted considerable attention in various fields such as organic synthesis and medical care. For the development of high-performance photosensitizers, highly efficient and persistent singlet oxygen generators (1O2) having a high oxidation tolerance are strongly required. This study presents a detailed investigation of dithieno[3,2-b:2′,3′-d]arsole-fluorene copolymer for its 1O2 generation ability and application as a photooxidation catalyst in vital organic reactions. Photoirradiation of an air-saturated solution of the polymer generates 1O2, which was detected by 1O2 scavengers such as dihydronaphthoquinone and diphenylisobenzofuran. The polymer photosensitizer was completely stable in the presence of the strong oxidant 1O2. The photosensitizer showed the highest quantum yield of 1O2 generation (Φ = 0.54) in single-component main-chain type π-conjugated polymers. The quantum yield of the arsenic-free analog of the polymer-bithiophene-fluorene copolymer-was significantly lower (Φ = 0.14), suggesting that the heavy-atom effect of arsenic can improve the efficiency of intersystem crossing (ISC) from the singlet excited state to the triplet excited state of the photosensitizer. In addition, when utilized as a recyclable photocatalyst for the oxidation reaction, the photosensitizer exhibited excellent oxidation resistance without losing its recognizable catalytic activity. Finally, we demonstrated the release of 1O2 into the air by a film of the present polymer. Persistent 1O2 generation was observed on film irradiation without polymer decomposition These results suggested that the polymer exhibited excellent oxidation resistance in solution as well as in the solid state. The present mol. design concept of the photosensitizer using the main group element can facilitate the development of further functional optical materials. In the experimental materials used by the author, we found Triacetonamine(cas: 826-36-8Synthetic Route of C9H17NO)

Triacetonamine(cas: 826-36-8) 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 C9H17NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Ishag, Abd Elaziz Sulieman Ahmed; Abdelbagi, Azhari Omer; Hammad, Ahmed Mohammed Ali; Elsheikh, Elsiddig Ahmed Elmustafa; Hur, Jang-Hyun published an article on February 28 ,2019. The article was titled 《Photodegradation of chlorpyrifos, malathion, and dimethoate by sunlight in the Sudan》, and you may find the article in Environmental Earth Sciences.Application In Synthesis of Triacetonamine The information in the text is summarized as follows:

The potential of sunlight photolysis in remediation of pesticide-polluted soils in Sudan was studied. Chlorpyrifos, malathion and dimethoate, common pollutants, were exposed to sunlight over glass and soil surfaces with periodic samples drawn for GC and GC-MS anal. Photo-degradation followed a biphasic model. Alpha half-lives of direct photolysis over glass surface range between 1.99 and 9.36 days while the range in soil surfaces is 1.88-10.77 days. Resp. values for indirect photolysis with βcarotene are 0.96-2.40 days whereas for benzophenone are 0.38-2.37 days (not including malathion as starting material was completely lost after 3 days). Values for soil β-carotene sensitized photolysis are 0.85-4.02 days while resp. values for soil benzophenone sensitized photolysis are 0.88-3.74 days. Metrol. factors did not have a significant impact on photolysis rates. No photoproducts detected in direct photolysis. However, many photoproducts were detected on the indirect sets. Photo-degradation efficiency can be ordered as; benzophenone > β-carotene > direct exposure. In the experiment, the researchers used many compounds, for example, Triacetonamine(cas: 826-36-8Application In Synthesis of Triacetonamine)

Triacetonamine(cas: 826-36-8) 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.Application In Synthesis of Triacetonamine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem