Category: amides-buliding-blocks

Dealkenylative Alkynylation Using Catalytic Fe^II and Vitamin C was written by Swain, Manisha;Bunnell, Thomas B.;Kim, Jacob;Kwon, Ohyun. And the article was included in Journal of the American Chemical Society in 2022.Safety of 1,3-Dicyclohexylurea This article mentions the following:

In this paper, synthesis of alkyl-tethered alkynes, e.g. I through ozone-mediated and Fe^II-catalyzed dealkenylative alkynylation of unactivated alkenes in presence of alkynyl sulfones was reported. This one-pot reaction, which employed a combination of a catalytic Fe^II salt and L-ascorbic acid, proceeded under mild conditions with good efficiency, high stereoselectivity, and broad functional group compatibility. In contrast to previous Fe^II-mediated reductive fragmentation of α-methoxyhydroperoxides, Fe^II-catalyzed process was devised through a thorough kinetic anal. of multiple competing radical (redox) pathways. The potential of this dealkenylative alkynylation through multiple post-synthetic transformations and late-stage diversifications of complex mols., including natural products and pharmaceuticals was highlighted. In the experiment, the researchers used many compounds, for example, 1,3-Dicyclohexylurea (cas: 2387-23-7Safety of 1,3-Dicyclohexylurea).

1,3-Dicyclohexylurea (cas: 2387-23-7) belongs to amides. Compared to amines, amides are very weak bases and do not have clearly defined acid–base properties in water. On the other hand, amides are much stronger bases than esters, aldehydes, and ketones. Ionic, or saltlike, amides are strongly alkaline compounds ordinarily made by treating ammonia, an amine, or a covalent amide with a reactive metal such as sodium.Safety of 1,3-Dicyclohexylurea

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Visible light-driven [3 + 3] annulation reaction of 2H-azirines with Huisgen zwitterions and synthesis of 1,2,4-triazines was written by Cao, Shixuan;Tang, Tong;Li, Jiatian;He, Zhengjie. And the article was included in Organic Chemistry Frontiers in 2022.Recommanded Product: 116332-61-7 This article mentions the following:

A visible light-driven [3 + 3] annulation reaction of 2H-azirines with in-situ generated Huisgen zwitterions from azodicarboxylates and phosphines was herein described. Under very mild conditions and irradiation of blue LED light, disubstituted 2H-azirines readily undergo a formal [3 + 3] annulation reaction with in-situ generated Huisgen zwitterions, affording polysubstituted dihydro-1,2,4-triazines in 51-97% yields with a broad substrate scope. Mechanistic studies unveil that this annulation reaction proceeded through a cascade sequence of nucleophilic addition, light-driven 1,3-ester migration and aza-Wittig-like cyclization. The light-driven ester migration step was believed to be a photochem. process of an intramol. electron donor-acceptor (EDA) complex. In the experiment, the researchers used many compounds, for example, N-Methoxy-N-methyl-4-(trifluoromethyl)benzamide (cas: 116332-61-7Recommanded Product: 116332-61-7).

N-Methoxy-N-methyl-4-(trifluoromethyl)benzamide (cas: 116332-61-7) belongs to amides. Compared to amines, amides are very weak bases and do not have clearly defined acid–base properties in water. On the other hand, amides are much stronger bases than esters, aldehydes, and ketones. The presence of the amide group –C(=O)N– is generally easily established, at least in small molecules. It can be distinguished from nitro and cyano groups in IR spectra. Amides exhibit a moderately intense νCO band near 1650 cm−1. By 1H NMR spectroscopy, CONHR signals occur at low fields. In X-ray crystallography, the C(=O)N center together with the three immediately adjacent atoms characteristically define a plane.Recommanded Product: 116332-61-7

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Palladium-Catalyzed α-Arylation of Vinylogous Esters for the Synthesis of γ,γ-Disubstituted Cyclohexenones was written by Johnson, Thomas;Pultar, Felix;Menke, Friedericke;Lautens, Mark. And the article was included in Organic Letters in 2016.Category: amides-buliding-blocks This article mentions the following:

A palladium-catalyzed α-arylation of cyclic vinylogous esters to form products that are converted in one step to γ-alkyl-γ-aryl-substituted cyclohexenones is reported. This Pd-catalyzed reaction proceeds at room temperature, is generally high-yielding, and uses an amount of a com. available catalyst as low as 0.25 mol %. The scope of aryl bromides is particularly broad, and alkenyl bromides can also be used. This two-step protocol, comprising α-arylation and reductive transposition, can be performed in one pot and is applicable to gram-scale synthesis. In the experiment, the researchers used many compounds, for example, 4-Bromo-N-methoxy-N-methylbenzamide (cas: 192436-83-2Category: amides-buliding-blocks).

4-Bromo-N-methoxy-N-methylbenzamide (cas: 192436-83-2) belongs to amides. Amides include many other important biological compounds, as well as many drugs like paracetamol, penicillin and LSD. Low-molecular-weight amides, such as dimethylformamide, are common solvents. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Development of [¹⁸F]Maleimide-Based Glycogen Synthase Kinase-3β Ligands for Positron Emission Tomography Imaging was written by Hu, Kongzhen;Patnaik, Debasis;Collier, Thomas Lee;Lee, Katarzyna N.;Gao, Han;Swoyer, Matthew R.;Rotstein, Benjamin H.;Krishnan, Hema S.;Liang, Steven H.;Wang, Jin;Yan, Zhiqiang;Hooker, Jacob M.;Vasdev, Neil;Haggarty, Stephen J.;Ngai, Ming-Yu. And the article was included in ACS Medicinal Chemistry Letters in 2017.Computed Properties of C8H8ClNO This article mentions the following:

Dysregulation of glycogen synthase kinase-3β (GSK-3β) is implicated in the pathogenesis of neurodegenerative and psychiatric disorders. Thus, development of GSK-3β radiotracers for positron emission tomog. (PET) imaging is of paramount importance, because such a noninvasive imaging technique would allow better understanding of the link between the activity of GSK-3β and central nervous system disorders in living organisms, and it would enable early detection of the enzyme’s aberrant activity. Herein, we report the synthesis and biol. evaluation of a series of fluorine-substituted maleimide derivatives that are high-affinity GSK-3β inhibitors. Radiosynthesis of a potential GSK-3β tracer [¹⁸F]10a is achieved. Preliminary in vivo PET imaging studies in rodents show moderate brain uptake, although no saturable binding was observed in the brain. Further refinement of the lead scaffold to develop potent [¹⁸F]-labeled GSK-3 radiotracers for PET imaging of the central nervous system is warranted. In the experiment, the researchers used many compounds, for example, 2-(2-Chlorophenyl)acetamide (cas: 10268-06-1Computed Properties of C8H8ClNO).

2-(2-Chlorophenyl)acetamide (cas: 10268-06-1) belongs to amides. The amide group is called a peptide bond when it is part of the main chain of a protein, and an isopeptide bond when it occurs in a side chain, such as in the amino acids asparagine and glutamine. Amides are not in general accessible by the direct condensation of amines with carboxylic acids for two reasons: first, both components are readily deactivated by a transfer of a proton from the acid to the amine and second, the hydroxy unit on the carbonyl of the acid is a relatively poor leaving group. Nevertheless, the formation of five- and six-membered rings is often surprisingly simple provided that other factors can be brought into play to assist in the condensation.Computed Properties of C8H8ClNO

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Asymmetric Copper-Catalyzed Intermolecular Aminoarylation of Styrenes: Efficient Access to Optical 2,2-Diarylethylamines was written by Wang, Dinghai;Wu, Lianqian;Wang, Fei;Wan, Xiaolong;Chen, Pinhong;Lin, Zhenyang;Liu, Guosheng. And the article was included in Journal of the American Chemical Society in 2017.Related Products of 5339-69-5 This article mentions the following:

We have developed a copper-catalyzed enantioselective intermol. aminoarylation of alkenes using a novel N-fluoro-N-alkylsulfonamide as the amine reagent, which could react with the Cu(I) catalyst to release a related amino radical. After addition to styrene, the generated benzylic radical could couple with a chiral L*Cu^IIAr complex to achieve enantioselective arylation. Various optical 2,2-diarylethylamines were efficiently synthesized from simple styrenes with high enantioselectivity, and these products can serve as valuable synthons toward bioactive mols.’ synthesis. In the experiment, the researchers used many compounds, for example, N-Isopropylbenzenesulfonamide (cas: 5339-69-5Related Products of 5339-69-5).

N-Isopropylbenzenesulfonamide (cas: 5339-69-5) belongs to amides. Compared to amines, amides are very weak bases and do not have clearly defined acid–base properties in water. On the other hand, amides are much stronger bases than esters, aldehydes, and ketones. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.Related Products of 5339-69-5

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Aloe-emodin, a naturally occurring anthraquinone, is a highly potent mast cell stabilizer through activating mitochondrial calcium uniporter was written by Gao, Yuan;Zhang, Xiaoyu;Li, Ximeng;Qi, Ruijuan;Han, Yixin;Kang, Yuan;Cai, Runlan;Peng, Cheng;Qi, Yun. And the article was included in Biochemical Pharmacology (Amsterdam, Netherlands) in 2021.Product Details of 53902-12-8 This article mentions the following:

Mast cells play a fundamental role in immune system. Upon stimulation, they are activated via IgE dependent or independent pathway and then release granules which contain plenty of preformed constituents. Mast cell stabilizers are commonly used clin. for inhibiting the degranulation of mast cells. In the current study, we firstly identified aloe-emodin, a naturally occurring anthraquinone, was a prominent mast cell stabilizer. It could strikingly dampen IgE/FcεRI- and MAS-related G protein coupled receptor (Mrgpr)-mediated mast cell degranulation in vitro and in vivo. Mechanism study indicated that aloe-emodin rapidly and reversibly decreased cytosolic Ca2+ (Ca2+[c]) concentration through enhancing the mitochondrial Ca2+ (Ca2+[m]) uptake. After genetically silencing or pharmacol. inhibiting mitochondrial calcium uniporter (MCU), the effects of aloe-emodin on the Ca2+[c] level and mast cell degranulation were significantly weakened. In contrast to six clin. drugs with mast cell stabilizing properties (amlexanox, tranilast, ketotifen, cromolyn disodium salt, dexamethasone and pimecrolimus), aloe-emodin showed an impressive and potent inhibitory action on the mast cell degranulation. Collectively, aloe-emodin is a highly potent mast cell stabilizer. By directly activating MCU, it decreases Ca2+[c] level to suppress mast cell degranulation. Our study may provide a promising candidate for the treatment of mast cell activation-related diseases. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Product Details of 53902-12-8).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) belongs to amides. The amide group is called a peptide bond when it is part of the main chain of a protein, and an isopeptide bond when it occurs in a side chain, such as in the amino acids asparagine and glutamine. In simple aromatic amides, fragmentation occurs on both sides of the carbonyl group. If a hydrogen is available in N-substituted aromatic amides, it tends to migrate and form an aromatic amine and the loss of a ketene.Product Details of 53902-12-8

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

A comparative study of several activator in enzyme peroxide one bath low temperature pretreatment was written by Zhu, Jun-ping. And the article was included in Yinran Zhuji in 2015.Application of 10543-57-4 This article mentions the following:

The application effect of four hydrogen peroxide activators in enzyme one bath pretreatment was investigated. The results showed that the effect of TAED was good. Enzyme peroxide one bath could reduce the alkali dosage and reduce the burden on sewage treatment. The application process was as follows: gray fabric padding the first working fluid (two-dip-two-nip, padding rate 90% ∼ 100%, the working fluid temperature 50 ∼ 55 °C) → curled batching (50 °C,12 h) → padding the second working fluid (two-dip-two-nip, padding rate 90% ∼ 100%, the working fluid temperature 40 °C) → steaming (80 °C,10 min) → washing → drying. The first working fluid: KDN scouring enzyme 2 g/L, low temperature scouring penetrant GR-01 10 g/L, hydrogen peroxide solution 36 mL/L, activator 18 g/L, pH = 8. The second working fluid: low temperature scouring penetrant GR-01 10 g/L, hydrogen peroxide solution 44 mL/L, activator 22 g/L, pH = 8 ∼ 9. In the experiment, the researchers used many compounds, for example, N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4Application of 10543-57-4).

N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4) belongs to amides. The amide group is called a peptide bond when it is part of the main chain of a protein, and an isopeptide bond when it occurs in a side chain, such as in the amino acids asparagine and glutamine. In simple aromatic amides, fragmentation occurs on both sides of the carbonyl group. If a hydrogen is available in N-substituted aromatic amides, it tends to migrate and form an aromatic amine and the loss of a ketene.Application of 10543-57-4

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Prediction of permeability across intestinal cell monolayers for 219 disparate chemicals using in vitro experimental coefficients in a pH gradient system and in silico analyses by trivariate linear regressions and machine learning was written by Kamiya, Yusuke;Omura, Asuka;Hayasaka, Riku;Saito, Rie;Sano, Izumi;Handa, Kentaro;Ohori, Junya;Kitajima, Masato;Shono, Fumiaki;Funatsu, Kimito;Yamazaki, Hiroshi. And the article was included in Biochemical Pharmacology (Amsterdam, Netherlands) in 2021.Related Products of 53902-12-8 This article mentions the following:

For medicines, the apparent membrane permeability coefficients (Papp) across human colorectal carcinoma cell line (Caco-2) monolayers under a pH gradient generally correlate with the fraction absorbed after oral intake. Furthermore, the in vitro Papp values of 29 industrial chems. were found to have an inverse association with their reported no-observed effect levels for hepatotoxicity in rats. In the current study, we expanded our influx permeability predictions for the 90 previously investigated chems. to both influx and efflux permeability predictions for 207 diverse primary compounds, along with those for 23 secondary compounds Trivariate linear regression anal. found that the observed influx and efflux logPapp values determined by in vitro experiments significantly correlated with mol. weights and the octanol-water distribution coefficients at apical and basal pH levels (pH 6.0 and 7.4, resp.) (apical to basal, r = 0.76, n = 198; and basal to apical, r = 0.77, n = 202); the distribution coefficients were estimated in silico. Further, prediction accuracy was enhanced by applying a light gradient boosting machine learning system (LightGBM) to estimate influx and efflux logPapp values that incorporated 17 and 19 in silico chem. descriptors (r = 0.83-0.84, p < 0.001). The determination in vitro and/or prediction in silico of permeability coefficients across intestinal cell monolayers of a diverse range of industrial chems./food components/medicines could contribute to the safety evaluations of oral intakes of general chems. in humans. Such new alternative methods could also reduce the need for animal testing during toxicity assessment. In the experiment, the researchers used many compounds, for example, 2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8Related Products of 53902-12-8).

2-(3-(3,4-Dimethoxyphenyl)acrylamido)benzoic acid (cas: 53902-12-8) belongs to amides. Compared to amines, amides are very weak bases and do not have clearly defined acid–base properties in water. On the other hand, amides are much stronger bases than esters, aldehydes, and ketones. Ionic, or saltlike, amides are strongly alkaline compounds ordinarily made by treating ammonia, an amine, or a covalent amide with a reactive metal such as sodium.Related Products of 53902-12-8

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Novel applications of eureco RP 103 was written by Garaffa, Roberto;Warunek, Magda;Findlay, Paul;Pears, David;Scullion, Lisa;Hughes, Melanie. And the article was included in IP.com Journal in 2016.SDS of cas: 10543-57-4 This article mentions the following:

Eureco RP 103 is a new free flowing, boron free particle containing 6-phthalimidoperoxyhexanoic acid (PAP). The particle is stable on its own and when formulated with various other media under ambient and elevated temperature and humidity conditions. It is a versatile material that can be used in a wide range of different product formulations and applications. In the experiment, the researchers used many compounds, for example, N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4SDS of cas: 10543-57-4).

N,N-(Ethane-1,2-diyl)bis(N-acetylacetamide) (cas: 10543-57-4) belongs to amides. The amide group is called a peptide bond when it is part of the main chain of a protein, and an isopeptide bond when it occurs in a side chain, such as in the amino acids asparagine and glutamine. Amides can be freed from solvent or water by drying below their melting points. These purifications can also be used for sulfonamides and acid hydrazides.SDS of cas: 10543-57-4

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

The analgesic properties of some substituted salicylamide derivatives was written by Carron, M.;Tabart, J.;Jullien, Mrs.. And the article was included in Therapie in 1952.Related Products of 19311-91-2 This article mentions the following:

Derivatives of salicylamide (I) were prepared; they had general formulas C₆H₄OH.CONRR’ or C₆H₄CONH₂. OR”. Their lethal doses (per os) and analgesic effects were determined by the Armour and Smith method (J. Pharm. Exptl. Therap. 72, 74, 1941). Introduction of hydrosol. groups, methoxylation, and acetylation of the phenolic function lowered the analgesic power; ethoxylation of the same increased it. Substitution of amide H by alkyls activated the analgesic effect from Et to iso-Pr, but Me and Bu derivatives had low activities. Hydrosol. functions introduced on the amide did not modify the effect of the products. Joining 2 I mols by a C₃ chain increased its effect, but a C₁ or C₂ linkage lowered the activity of the compounds Min. analgesic doses and lethal doses of the most active derivatives compared with acetylsalicylic acid (II) were: I 0.3, 0.6; N-diethyl-I 0.15, 0.85; o-ethoxybenzamide 0.2, 0.7; o-acetylsalicylureide 0.2, 0.3; methylol-I 0.24, 0.85; N-isopropyl-I 0.25, 0.65; propylenebis-I 0.26, 0.95; and II 0.4, 0.83 g./kg. weight of mice. In the experiment, the researchers used many compounds, for example, N,N-Diethylsalicylamide (cas: 19311-91-2Related Products of 19311-91-2).

N,N-Diethylsalicylamide (cas: 19311-91-2) belongs to amides. The amide group is called a peptide bond when it is part of the main chain of a protein, and an isopeptide bond when it occurs in a side chain, such as in the amino acids asparagine and glutamine. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.Related Products of 19311-91-2

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics