Day: October 13, 2022

Application 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: 194726-40-4Application 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.Application of 194726-40-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Name: (S)-2-Ethylpiperidine hydrochlorideOn 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: 558479-16-6Name: (S)-2-Ethylpiperidine hydrochloride)

(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.Name: (S)-2-Ethylpiperidine hydrochloride

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.Electric Literature of C9H17NO 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: 826-36-8Electric Literature of C9H17NO) 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.Electric Literature of C9H17NO

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》.Related Products of 109384-19-2 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: 109384-19-2Related Products of 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.Related Products of 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Recommanded Product: 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: 118511-81-2Recommanded Product: 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. Recommanded Product: 1-(Piperidin-4-yl)-1H-indole

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Electric Literature 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: 826-36-8Electric Literature 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.Electric Literature 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.Recommanded Product: 826-36-8 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: 826-36-8Recommanded Product: 826-36-8)

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.Recommanded Product: 826-36-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Liao, Chenzhong; Nicklaus, Marc C. published their research in Journal of Chemical Information and Modeling on December 31 ,2009. The article was titled 《Comparison of Nine Programs Predicting pKa Values of Pharmaceutical Substances》.SDS of cas: 1690-72-8 The article contains the following contents:

Knowledge of the possible ionization states of a pharmaceutical substance, embodied in the pKa values (logarithm of the acid dissociation constant), is vital for understanding many properties essential to drug development. We compare nine com. available or free programs for predicting ionization constants Eight of these programs are based on empirical methods: ACD/pKa DB 12.0, ADME Boxes 4.9, ADMET Predictor 3.0, Epik 1.6, Marvin 5.1.4, Pallas pKalc Net 2.0, Pipeline Pilot 5.0, and SPARC 4.2; one program is based on a quantum chem. method: Jaguar 7.5. We compared their performances by applying them to 197 pharmaceutical substances with 261 carefully determined and highly reliable exptl. pKa values from a literature source. The programs ADME Boxes 4.9, ACD/pKa DB 12.0, and SPARC 4.2 ranked as the top three with mean absolute deviations of 0.389, 0.478, and 0.651 and r2 values of 0.944, 0.908, and 0.894, resp. ACD/pKa DB 12.0 predicted all sites, whereas ADME Boxes 4.9 and SPARC 4.2 failed to predict 5 and 18 sites, resp. The performance of the quantum chem.-based program Jaguar 7.5 was not as expected, with a mean absolute deviation of 1.283 and an r2 value of 0.579, indicating the potential for further development of this type of approach to pKa prediction. In the part of experimental materials, we found many familiar compounds, such as Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8SDS of cas: 1690-72-8)

Methyl 1-methylpiperidine-3-carboxylate(cas: 1690-72-8) 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.SDS of cas: 1690-72-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Liu, Li; Li, Yuxin; Pang, Yaqian; Lan, Yeqing; Zhou, Lixiang published their research in Chemical Engineering Journal (Amsterdam, Netherlands) on December 1 ,2020. The article was titled 《Activation of peroxymonosulfate with CuCo2O4@kaolin for efficient degradation of phenacetin》.Reference of Triacetonamine The article contains the following contents:

CuCo2O4@kaolin was successfully synthesized by a sol-gel method and used as a heterogeneous catalyst to activate peroxymonosulfate (PMS) for the degradation of phenacetin (PNT). The results demonstrated that 10 mg/L PNT was completely decomposed by 1 mM PMS activated with 0.1 g/L CuCo2O4@kaolin within 15 min at initial pH 7. CuCo2O4@kaolin exhibited the best excellent catalytic performance among the tested catalysts, and the pseudo-first-order rate constants of PNT degradation were CuCo2O4@kaolin (0.40 min-1) > CuCo2O4 (0.22 min-1) > Co3O4@kaolin (0.10 min-1) > CuO@kaolin (0.08 min-1) > kaolin (0.02 min-1). CuCo2O4@kaolin also possessed superior stability, and the degradation efficiency of PNT declined from 100% in the first round to 80% in the fourth round. Nevertheless, a simple calcinating treatment (20 min) after the third round could restore its catalytic activity substantially and 95% removal of PNT was realized, 15% higher compared to without treatment. ·OH, SO4·-, and 1O2 were the reactive oxygen species driving the PNT degradation Based on the results mentioned above, characterizations of CuCo2O4@kaolin, and intermediates of PNT degradation, the possible pathways and underlying mechanisms of the PNT degradation in the CuCo2O4@kaolin/PMS system were deduced. CuCo2O4@kaolin/PMS had a universal degradation potential toward various organic pollutants, and the degradation efficiencies of sulfisoxazole, p-nitrophenol, chloramphenicol, and 2,4,6-Trichlorophenol reached 95-100% within 5-45 min. Thus, this work provides a novel and efficient PMS activator through an eco-friendly synthetic route, and it may be put into practice to degrade organic matter in wastewater.Triacetonamine(cas: 826-36-8Reference 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.Reference of Triacetonamine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

The author of 《One-pot synthesis of novel tert-butyl-4-substituted phenyl-1H-1,2,3-triazolo piperazine/piperidine carboxylates, potential GPR119 agonists》 were Bashetti, Nagaraju; Shanmukha Kumar, J. V.; Seelam, Naresh Varma; Prasanna, B.; Mintz, Akiva; Damuka, Naresh; Devanathan, Sriram; Solingapuram Sai, Kiran Kumar. And the article was published in Bioorganic & Medicinal Chemistry Letters in 2019. Quality Control of tert-Butyl 4-hydroxypiperidine-1-carboxylate The author mentioned the following in the article:

We have synthesized a new series of 1,2,3-triazolo piperazine and piperidine carboxylate derivatives using a simple and one-pot click chem. with significantly reduced reaction times (∼5 min) and enhanced reaction yields (∼95-98%). The fourteen novel compounds thus synthesized were tested for ability to target GPR119, a G-protein coupled target receptor that plays critical role in regulation of type-2 diabetes mellitus. Four analogs demonstrated similar or better EC50 values over previously reported AR231453 activity towards GPR119. The experimental process involved the reaction of tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Quality Control of 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.Quality Control of tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem