Category: 2873-29-2

Reference of 2873-29-2, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 2873-29-2, Name is (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate, SMILES is O=C(OC[C@@H]1[C@@H](OC(C)=O)[C@H](OC(C)=O)C=CO1)C, belongs to piperidines compound. In a article, author is Sharma, Rajni, introduce new discover of the category.

Khellinoflavanone, a Semisynthetic Derivative of Khellin, Overcomes Benzo[a] pyrene Toxicity in Human Normal and Cancer Cells That Express CYP1A1

Cytochrome P450 family 1 (CYP1) enzymes catalyze the metabolic activation of environmental procarcinogens such as benzo[a] pyrene, B[a] P, into carcinogens, which initiates the process of carcinogenesis. Thus, stopping the metabolic activation of procarcinogens can possibly prevent the onset of cancer. Several natural products have been reported to show unique ability in inhibiting CYP1 enzymes. We found that khellin, a naturally occurring furanochromone from Ammi visnaga, inhibits CYP1A1 enzyme with an IC50 value of 4.02 mu M in CYP1A1-overexpressing human HEK293 suspension cells. To further explore this natural product for discovery of more potent and selective CYP1A1 inhibitors, two sets of semisynthetic derivatives were prepared. Treatment of khellin with alkali results in opening of a pyrone ring, yielding khellinone (2). Claisen-Schmidt condensation of khellinone (2) with various aldehydes in presence of potassium hydroxide, at room temperature, provides a series of furanochalcones 3a-v (khellinochalcones). Treatment of khellinone (2) with aryl aldehydes in the presence of piperidine, under reflux, affords the flavanone series of compounds 4a-p (khellinoflavanones). The khellinoflavanone 4l potently inhibited CYP1A1 with an IC50 value of 140 nM in live cells, with 170fold selectivity over CYP1B1 (IC50 for CYP1B1 = 23.8 mu M). Compound 4l at 3x IC50 concentration for inhibition of CYP1A1 completely protected HEK293 cells from CYP1A1-mediated B[a] P toxicity. Lung cancer cells, A549 (p53+) and Calu-1 (p53null), blocked in growth at the S-phase by B[a] P were restored into the cell cycle by compound 4l. The results presented herein strongly indicate the potential of these khellin derivatives for further development as cancer chemopreventive agents.

Reference of 2873-29-2, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 2873-29-2.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. In an article, author is Ogura, Akihiro, once mentioned the application of 2873-29-2, Name is (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate, molecular formula is C12H16O7, molecular weight is 272.25, MDL number is MFCD00063253, category is piperidines. Now introduce a scientific discovery about this category, Category: piperidines.

Red-Light-Mediated Barton-McCombie Reaction

A red-light-mediated Barton-McCombie reaction is described, in which chlorophyll a is used as a photocatalyst and tris(trimethylsilyl)silane or Hantzsch ester is used as the hydrogen source. The reaction can be performed with a set of easily available equipment and reagents, and a variety of linear and cyclic xanthates could be applied. In contrast to the traditional conditions, the reaction does not involve toxic organotin or an explosive radical initiator. The reaction mechanism was analyzed both by experiments and computation, and it was suggested that the radical chain mechanism initiated by excitation of complex followed by charge transfer is likely to be operative.

Do you like my blog? If you like, you can also browse other articles about this kind. Thanks for taking the time to read the blog about 2873-29-2, Category: piperidines.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

Chemistry, like all the natural sciences, Formula: C12H16O7, begins with the direct observation of nature— in this case, of matter.2873-29-2, Name is (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate, SMILES is O=C(OC[C@@H]1[C@@H](OC(C)=O)[C@H](OC(C)=O)C=CO1)C, belongs to piperidines compound. In a document, author is Rickertsen, Dillon R. L., introduce the new discover.

Traceless Redox-Annulations of Alicyclic Amines

Amines such as 1,2,3,4-tetrahydroisoquinoline undergo redox–neutral annulations with ortho-(nitromethyl)benzaldehyde. Benzoic- acid acts as a promoter in these reactions, which involve concurrent amine alpha-C-H bond and N-H bond functionalization. Subsequent removal of the nitro group provides access to tetrahydroprotoberberines not accessible via typical redox-annulations. Also reported are decarboxylative annulations of ortho-(nitromethyl)benzaldehyde with proline and pipecolic acid.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions. you can also check out more blogs about 2873-29-2. Formula: C12H16O7.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. 2873-29-2, Name is (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate, SMILES is O=C(OC[C@@H]1[C@@H](OC(C)=O)[C@H](OC(C)=O)C=CO1)C, in an article , author is Anderson, James C., once mentioned of 2873-29-2, Category: piperidines.

Asymmetric synthesis of piperidines using the nitro-Mannich reaction

A method for the synthesis of functionalized piperidines containing 3 contiguous stereocentres in the 2-,3- and 4- positions uses a diastereoselective nitro-Mannich to control stereochemistry. The nitro-Mannich reaction between a beta-aryl/heteroaryl substituted nitroalkanes and glyoxylate imine provides beta-nitro-amines with good selectivity (70:30 to >95:5) for the syn, anti-diastereoisomers. Reductive cyclisation with BF3 center dot OEt2 and Et3SiH gave, after purification, stereochemically pure piperidines in 19-57% yield for ten examples with different 4-aryl/heteroaryl substituents. (C) 2020 Elsevier Ltd. All rights reserved.

Interested yet? Read on for other articles about 2873-29-2, you can contact me at any time and look forward to more communication. Category: piperidines.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time. 2873-29-2, Name is (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate, formurla is C12H16O7. In a document, author is Abdelhameed, Ali S., introducing its new discovery. Recommanded Product: 2873-29-2.

Identification of Iminium Intermediates Generation in the Metabolism of Tepotinib Using LC-MS/MS: In Silico and Practical Approaches to Bioactivation Pathway Elucidation

Tepotinib (Tepmetko (TM), Merck) is a potent inhibitor of c-Met (mesenchymal-epithelial transition factor). In March 2020, tepotinib (TEP) was approved for use in Japan for the treatment of patients who suffered from non-small cell lung cancers (NSCLC) harboring an MET exon 14 skipping alteration and have progressed after platinum-based therapy. Practical and in silico experiments were used to screen for the metabolic profile and reactive intermediates of TEP. Knowing the bioactive center and structural alerts in the TEP structure helped in making targeted modifications to improve its safety. First, the prediction of metabolism vulnerable sites and reactivity metabolic pathways was performed using the StarDrop WhichP450 (TM) module and the online Xenosite reactivity predictor tool, respectively. Subsequently, in silico data were used as a guide for the in vitro practical work. Second, in vitro phase I metabolites of TEP were generated from human liver microsome (HLM) incubations. Testing for the generation of unstable reactive intermediates was performed using potassium cyanide as a capturing agent forming stable cyano adduct that can be characterized and identified using liquid chromatography tandem mass spectrometry (LC-MS/MS). Third, in silico toxicity assessment of TEP metabolites was performed, and structural modification was proposed to decrease their side effects and to validate the proposed bioactivation pathway using the DEREK software. Four TEP phase I metabolites and four cyano adducts were characterized. The reactive intermediate generation mechanism of TEP may provide an explanation of its adverse reactions. The piperidine ring is considered a structural alert for toxicity as proposed by the DEREK software and a Xenosite reactivity model, which was confirmed by practical experiments. Steric hindrance or isosteric replacement at alpha-carbon of the piperidine ring stop the bioactivation sequence that was confirmed using the DEREK software. More drug discovery studies can be performed using this perception permitting the design of new drugs with an increased safety profile. To our knowledge, this is the first study for the identification of in vitro phase I metabolites and reactive intermediates in addition to toxicological properties of the metabolites for TEP that will be helpful for the evaluation of TEP side effects and drug-drug interactions in TEP-treated patients.

If you are hungry for even more, make sure to check my other article about 2873-29-2, Recommanded Product: 2873-29-2.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. 2873-29-2, Name is (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate, SMILES is O=C(OC[C@@H]1[C@@H](OC(C)=O)[C@H](OC(C)=O)C=CO1)C, in an article , author is Larson, Nicholas R., once mentioned of 2873-29-2, Computed Properties of C12H16O7.

Heterocyclic Amine-Induced Feeding Deterrence and Antennal Response of Honey Bees

Simple Summary This study examined the behavioral and antennal effects of heterocyclic amines (HCAs) on forager honey bees. Behavioral changes related to feeding were initially characterized using a video-tracking protocol in which individual foragers were exposed to HCA-treated food sources within a Petri dish arena. The most efficacious HCA was then tested in a field study using a high-tunnel arena to determine whether repellent effects could be observed on a larger number of foragers to a treated food source. The same HCA was then tested in the field on both melon flowers and knapweed bundles to observe whether repellency was conserved in a more agriculturally realistic scenario. Finally, electroantennogram (EAG) experiments were conducted to document whether the honey bee olfactory system was detecting these compounds. These findings suggest that HCAs could provide an active approach to deter honey bee foragers from feeding on treated agricultural crops. The productivity and survival of managed honey bee colonies is negatively impacted by a diverse array of interacting factors, including exposure to agrochemicals, such as pesticides. This study investigated the use of volatile heterocyclic amine (HCA) compounds as potential short-term repellents that could be employed as feeding deterrents to reduce the exposure of bees to pesticide-treated plants. Parent and substituted HCAs were screened for efficacy relative to the repellent N,N-diethyl-meta-toluamide (DEET) in laboratory and field experiments. Additionally, electroantennogram (EAG) recordings were conducted to determine the level of antennal response in bees. In video-tracking recordings, bees were observed to spend significantly less time with an HCA-treated food source than an untreated source. In a high-tunnel experiment, the HCA piperidine was incorporated in a feeding station and found to significantly reduce bee visitations relative to an untreated feeder. In field experiments, bee visitations were significantly reduced on melon flowers (Cucumis melo L.) and flowering knapweed (Centaurea stoebe L.) that were sprayed with a piperidine solution, relative to untreated plants. In EAG recordings, the HCAs elicited antennal responses that were significantly different from control or vehicle responses. Overall, this study provides evidence that HCAs can deter individual bees from food sources and suggests that this deterrence is the result of antennal olfactory detection. These findings warrant further study into structure-activity relationships that could lead to the development of short-term repellent compounds that are effective deterrents to reduce the contact of bees to pesticide-treated plants.

Interested yet? Read on for other articles about 2873-29-2, you can contact me at any time and look forward to more communication. Computed Properties of C12H16O7.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 2873-29-2, Name is (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate, molecular formula is C12H16O7. In an article, author is Kumar, Pradeep,once mentioned of 2873-29-2, Application In Synthesis of (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate.

Proline-Catalyzed Asymmetric -Amination in the Synthesis of Bioactive Molecules

The direct -amination of carbonyl compounds using organocatalysts represents a powerful and atom-economical tool for asymmetric C-N bond formation. We describe a complete account of -functionalization of carbonyl compounds, through iterative sequential -aminoxylation/amination using electrophilic O and N sources, as well as sequential -amination/HWE reaction for enantio- and diastereoselective synthesis of both syn – and anti -1,3-aminoalcohols and 1,3-diamines. Additionally this protocol is further extended for the easy construction of alkaloids such as indolizidine, pyrrolizidine, and quinolizidine fused-ring systems just by tuning the chain length of the aldehyde used as a starting material. This methodology provides further scope to extrapolate it for a variety of naturally occurring hydroxylated monocyclic and fused bicyclic pyrrolidine and piperidine based alkaloids such as lentiginosine, epi -lentiginosine, dihydroxypyrrolizidine, (+)-deoxoprosophylline and (-)-deoxoprosopinine alkaloids. Furthermore, we have also uncovered proline-catalyzed anti -selectivity for the synthesis of 1,2-amino alcohols in -amination of aldehyde and one-pot indium-mediated Barbier type allylation of -hydrazino aldehydes to accomplish the total synthesis of clavaminols, sphinganine and spisulosine with reduced number of steps and with high overall yields. 1 Introduction 2 Application in the Total Synthesis of Alkaloids 3 Conclusion

Interested yet? Keep reading other articles of 2873-29-2, you can contact me at any time and look forward to more communication. Application In Synthesis of (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

In an article, author is Huang, Huoming, once mentioned the application of 2873-29-2, Name is (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate, molecular formula is C12H16O7, molecular weight is 272.25, MDL number is MFCD00063253, category is piperidines. Now introduce a scientific discovery about this category, Application In Synthesis of (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate.

Design, Synthesis, and Structure-Activity Relationship Exploration of Alkyl/Phenylalkyl Piperidine Analogues as Novel Highly Potent and Selective mu Opioid Receptor Agonists

Pain was implicated in many diseases. Despite effectiveness to treat moderate to severe pain, opioid analgesics elicited many side effects, greatly limiting their prescription in clinics. Based on Ml, an active metabolite of tramadol, 3-((dimethylamino)methyl)-4-(3-hydroxyphenyl)piperidin-4-ol analogues were designed, synthesized, and evaluated in vitro. Among all the compounds tested, compound 23 was found to be a novel, highly selective, and potent MOR agonist (K-i (MOR) = 0.0034 nM, EC50 MOR = 0.68 nM, E-max = 206.5%; K-i (DOR) = 41.67 nM; K KOR = 7.9 nM). Structure-activity relationship exploration showed that the linker between the piperidine ring and the phenyl ring as well as substituent pattern of the phenyl ring played a pivotal role in binding affinity and selectivity. (3R, 4S)-23 (K-i (MOR )= 0.0021 +/- 0.0001 nM, EC50 (MOR) = 0.0013 +/- 0.0001 nM, E-max = 209.1 +/- 1.4%; K DoR = 18.4 +/- 0.7 nM, EC50 (DOR) = 74.5 +/- 2.8 nM, E-max= 267.1 +/- 1.4%; K-i (KOR) = 25.8 +/- 0.2 nM, EC50 (DOR) = 116.2 +/- 4.4 nM, E-max = 209.5 +/- 1.4%) had more potent activity for opioid receptors than its enantiomer (3S, 4R)-23 and was found to be a potent, highly selective MOR agonist with novel scaffold. High binding affinity and selectivity of (3R, 4S)-23 for MOR over KOR and DOR and its mechanism of activating MOR were proposed by docking and molecular dynamics simulations, respectively.

Do you like my blog? If you like, you can also browse other articles about this kind. Thanks for taking the time to read the blog about 2873-29-2, Application In Synthesis of (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. , SDS of cas: 2873-29-2, 2873-29-2, Name is (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate, molecular formula is C12H16O7, belongs to piperidines compound. In a document, author is Liu, Guodu, introduce the new discover.

Pyrrolidines and piperidines bearing chiral tertiary alcohols by nickel-catalyzed enantioselective reductive cyclization of N-alkynones

Pyrrolidines and piperidines are important building blocks in organic synthesis. Numerous methods exist for constructing substituted pyrrolidines and piperidines. However, efficient syntheses of pyrrolidines and piperidines bearing chiral tertiary alcohols are limited. Here we report an efficient enantioselective nickel-catalyzed intramolecular reductive cyclization of N-alkynones. A P-chiral bisphosphorus ligand DI-BIDIME is designed and applied in the synthesis of tertiary allylic siloxanes bearing pyrrolidine and piperidine rings in high yields and excellent enantioselectivities, with triethylsilane as reducing reagent. The highest turn over number achieved is 1000 (0.1 mol% catalyst loading) with > 99:1 er. This reaction provides a practical way to synthesize pyrrolidine and piperidine derivatives with chiral tertiary alcohols from easily accessible starting materials under mild conditions. The products can be scaled up and transformed to various useful chiral intermediates. The P-chiral bisphosphorus ligand developed in this study represents one of the few ligands for highly enantioselective cyclization of alkynones.

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 2873-29-2. SDS of cas: 2873-29-2.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem

 

In an article, author is Sandig-Predzymirska, Lesia, once mentioned the application of 2873-29-2, Name is (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate, molecular formula is C12H16O7, molecular weight is 272.25, MDL number is MFCD00063253, category is piperidines. Now introduce a scientific discovery about this category, Application In Synthesis of (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate.

The direct and reversible hydrogenation of activated aluminium supported by piperidine

The reversible hydrogenation of aminoalanes employing activated aluminium and piperidine has been explored. A selection of transition metal (TM) compounds have been investigated as additives for producing TM-activated aluminium (TM = Ti, Zr, Hf and Y). The effect of these additives on the activation of aluminium with respect to hydrogenation of an aluminium/piperidinoalane system has been studied. It has been shown that Ti, Zr and Hf can efficiently promote the activation of aluminium for its hydrogenation. The experiments performed showed that the TM activity for the piperidinoalane formation decreases in the order Zr > Hf > Ti > Y. Using multinuclear NMR spectroscopy, the reversibility of this piperidinoalane-based hydrogenation system has been evidenced, demonstrating a potential pathway for hydrogen storage in aminoalanes. The syntheses of piperidinoalanes as well as their structural and spectroscopic characterisation are described. Single-crystal X-ray diffraction analyses of [pip(2)AlH](2) and [pip(3)Al](2) (pip = 1-piperidinyl, C5H10N) revealed dimers containing a central [AlN](2) unit.

Do you like my blog? If you like, you can also browse other articles about this kind. Thanks for taking the time to read the blog about 2873-29-2, Application In Synthesis of (2R,3S,4R)-2-(Acetoxymethyl)-3,4-dihydro-2H-pyran-3,4-diyl diacetate.

Reference:
Piperidine – Wikipedia,
,Piperidine | C5H11N – PubChem