Category: 27489-62-9

In 2018,Balaji, B. S.; Dalal, Neha published 《An expedient, chemoselective N-chloroacetylation of amino alcohols under metal-free bio-compatible conditions》.Green Chemistry Letters and Reviews published the findings.Related Products of 27489-62-9 The information in the text is summarized as follows:

For the first time, the authors report an efficient, highly chemoselective N-chloroacetylation of amino compounds (amino alcs., amino acids) by chloroacetyl chloride, without compromising its high reactivity, to give chloroacetamides in phosphate buffer within 20 min. A systematic study of the effects of buffers, metal salts and HCl scavengers to optimize the reaction conditions is described. Intermol. competitive reactions were carried out and showed that anilines and aliphatic amines could be selectively N-chloroacylated in the presence of alcs. and phenols. The acylated products were obtained in high yields and could be easily isolated without chromatog. separation This reaction represents the first example of a metal-free bio-compatible synthesis under neutral conditions. This method is eco-friendly, easily scalable and robust. Intramol. competitive reactions of aminoalcs. were further studied and gave various N-chloroacetamides in very good yields. Finally, this protocol was conveniently extended to the synthesis of ceramides. In the part of experimental materials, we found many familiar compounds, such as trans-4-Aminocyclohexanol(cas: 27489-62-9Related Products of 27489-62-9)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Aniline, ethanolamines, and several other amines are major industrial commodities used in making rubber, dyes, pharmaceuticals, and synthetic resins and fibres and for a host of other applications. Most of the numerous methods for the preparation of amines may be broadly divided into two groups: (1) chemical reduction (replacement of oxygen with hydrogen atoms in the molecule) of members of several other classes of organic nitrogen compounds and (2) reactions of ammonia or amines with organic compounds.Related Products of 27489-62-9

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《Discovery of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease》 was written by Leonard, Kristi A.; Madge, Lisa A.; Krawczuk, Paul J.; Wang, Aihua; Kreutter, Kevin D.; Bacani, Genesis M.; Chai, Wenying; Smith, Russell C.; Tichenor, Mark S.; Harris, Michael C.; Malaviya, Ravi; Seierstad, Mark; Johnson, Marguerite E.; Venable, Jennifer D.; Kim, Suzie; Hirst, Gavin C.; Mathur, Ashok S.; Rao, Tadimeti S.; Edwards, James P.; Rizzolio, Michele C.; Koudriakova, Tatiana. Reference of trans-4-Aminocyclohexanol And the article was included in Journal of Medicinal Chemistry in 2020. The article conveys some information:

To identify Janus kinase (JAK) inhibitors that selectively target gastrointestinal tissues with limited systemic exposures, a class of imidazopyrrolopyridines with a range of phys. properties was prepared and evaluated. We identified compounds with low intrinsic permeability and determined a correlation between permeability and physicochem. properties, clogP and tPSA, for a subset of compounds This low intrinsic permeability translated into compounds displaying high colonic exposure and low systemic exposure after oral dosing at 25 mg/kg in mouse. In a mouse PK/PD model, oral dosing of lead compound 2 demonstrated dose-dependent inhibition of pSTAT phosphorylation in colonic explants post-oral dose but low systemic exposure and no measurable systemic pharmacodynamic activity. We thus demonstrate the utility of JAK inhibitors with low intrinsic permeability as a feasible approach to develop gut-restricted, pharmacol. active mols. with a potential advantage over systemically available compounds that are limited by systemic on-target adverse events. The results came from multiple reactions, including the reaction of trans-4-Aminocyclohexanol(cas: 27489-62-9Reference of trans-4-Aminocyclohexanol)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Reference of trans-4-Aminocyclohexanol

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HPLC of Formula: 27489-62-9In 2021 ,《Thermodynamic Dissection of Potency and Selectivity of Cytosolic Hsp90 Inhibitors》 was published in Journal of Medicinal Chemistry. The article was written by Yoshimura, Chihoko; Nagatoishi, Satoru; Kuroda, Daisuke; Kodama, Yasuo; Uno, Takao; Kitade, Makoto; Chong-Takata, Khoontee; Oshiumi, Hiromi; Muraoka, Hiromi; Yamashita, Satoshi; Kawai, Yuichi; Ohkubo, Shuichi; Tsumoto, Kouhei. The article contains the following contents:

The cytosolic Hsp90-selective inhibitor TAS-116 has an acceptable safety profile and promising antitumor activity in clin. trials. We examined the binding characteristics of TAS-116 and its analogs to determine the impact of the ligand binding mode on selectivity for cytosolic Hsp90. Analyses of the co-crystal structure of Hsp90 and inhibitor TAS-116 suggest that TAS-116 interacts with the ATP-binding pocket, the ATP lid region, and the hydrophobic pocket. A competitive isothermal titration calorimetry anal. confirmed that a small fragment of TAS-116 (THS-510) docks into the lid region and hydrophobic pockets without binding to the ATP-binding pocket. THS-510 exhibited enthalpy-driven binding to Hsp90α and selectively inhibited cytosolic Hsp90 activity. The heat capacity change of THS-510 binding was pos., likely due to the induced conformational rearrangement of Hsp90. Thus, we concluded that interactions with the hydrophobic pocket of Hsp90 determine potency and selectivity of TAS-116 and derivatives for the cytosolic Hsp90 isoform. The experimental process involved the reaction of trans-4-Aminocyclohexanol(cas: 27489-62-9HPLC of Formula: 27489-62-9)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. To avoid the problem of multiple alkylation, methods have been devised for “blocking” substitution so that only one alkyl group is introduced. The Gabriel synthesis is one such method; it utilizes phthalimide, C6H4(CO)2NH, whose one acidic hydrogen atom has been removed upon the addition of a base such as KOH to form a salt.HPLC of Formula: 27489-62-9

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HPLC of Formula: 27489-62-9In 2019 ,《Design, synthesis, and biological evaluation of radioiodinated benzo[d]imidazole-quinoline derivatives for platelet-derived growth factor receptor β (PDGFRβ) imaging》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Effendi, Nurmaya; Mishiro, Kenji; Takarada, Takeshi; Yamada, Daisuke; Nishii, Ryuichi; Shiba, Kazuhiro; Kinuya, Seigo; Odani, Akira; Ogawa, Kazuma. The article conveys some information:

Several malignant tumors and fibrotic diseases are associated with PDGFRβ overexpression and excessive signaling, making this receptor attractive for mol. targeting and imaging approaches. A series of benzo[d]imidazole-quinoline derivatives were designed and synthesized to develop radioiodinated compounds as PDGFRβ-specific imaging probes. The structure activity relationship (SAR) evaluation of the designed compounds was performed. Among them, 2-[5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl]-8-(piperazin-1-yl)quinoline (5a) and 4-{2-[5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl]quinolin-8-yl}morpholine (5d) exhibited a relatively high PDGFRβ-TK inhibitory potency, whereas iodinated 5a derivative 5-iodo-2-[5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl]-8-(piperazin-1-yl)quinoline (8) exhibited a superior inhibitory potency as PDGFRβ inhibitor than iodinated 5d derivative 4-{5-iodo-2-[5-(2-methoxyethoxy)-1H-benzo[d]imidazol-1-yl]quinolin-8-yl}morpholine (11). Furthermore, [125I]8 and [125I]11 were synthesized and evaluated for PDGFRβ radioligand ability, both in vitro and in vivo. Cellular uptake experiments showed that [125I]8 had a higher uptake in BxPC3-luc cells as PDGFRβ-pos. cells than [125I]11. Incubation of [125I]8 after pretreatment of PDGFRβ ligands significantly reduced the uptake of [125I]8. In biodistribution experiments using tumor-bearing mice, [125I]8 accumulation in the tumor 1 h postinjection was higher than that of the benzo[d]imidazol-quinoline derivative [125I]IIQP, used in our previous research. These results indicate that [125I]8 could be a promising PDGFRβ imaging agent. Although its clin. application requires further structural modifications, the results obtained in this research may be useful for the development of PDGFRβ-specific radioligands. In the experimental materials used by the author, we found trans-4-Aminocyclohexanol(cas: 27489-62-9HPLC of Formula: 27489-62-9)

trans-4-Aminocyclohexanol(cas: 27489-62-9) 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.HPLC of Formula: 27489-62-9

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Reference of trans-4-AminocyclohexanolIn 2017 ,《Inhibitory Kappa B Kinase α (IKKα) Inhibitors That Recapitulate Their Selectivity in Cells against Isoform-Related Biomarkers》 appeared in Journal of Medicinal Chemistry. The author of the article were Anthony, Nahoum G.; Baiget, Jessica; Berretta, Giacomo; Boyd, Marie; Breen, David; Edwards, Joanne; Gamble, Carly; Gray, Alexander I.; Harvey, Alan L.; Hatziieremia, Sophia; Ho, Ka Ho; Huggan, Judith K.; Lang, Stuart; Llona-Minguez, Sabin; Luo, Jia Lin; McIntosh, Kathryn; Paul, Andrew; Plevin, Robin J.; Robertson, Murray N.; Scott, Rebecca; Suckling, Colin J.; Sutcliffe, Oliver B.; Young, Louise C.; Mackay, Simon P.. The article conveys some information:

IKKβ plays a central role in the canonical NF-kB pathway, which has been extensively characterized. The role of IKKα in the noncanonical NF-kB pathway, and indeed in the canonical pathway as a complex with IKKβ, is less well understood. One major reason for this is the absence of chem. tools designed as selective inhibitors for IKKα over IKKβ. Herein, we report for the first time a series of novel, potent, and selective inhibitors of IKKα. We demonstrate effective target engagement and selectivity with IKKα in U2OS cells through inhibition of IKKα-driven p100 phosphorylation in the noncanonical NF-kB pathway without affecting IKKβ-dependent IKappa-Bα loss in the canonical pathway. These compounds represent the first chem. tools that can be used to further characterize the role of IKKα in cellular signaling, to dissect this from IKKβ and to validate it in its own right as a target in inflammatory diseases. The experimental process involved the reaction of trans-4-Aminocyclohexanol(cas: 27489-62-9Reference of trans-4-Aminocyclohexanol)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Amine, any member of a family of nitrogen-containing organic compounds that is derived, either in principle or in practice, from ammonia (NH3). Naturally occurring amines include the alkaloids, which are present in certain plants; the catecholamine neurotransmitters (i.e., dopamine, epinephrine, and norepinephrine); and a local chemical mediator, histamine, that occurs in most animal tissues.Reference of trans-4-Aminocyclohexanol

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Application of 27489-62-9In 2019 ,《Synthesis and structure-activity relationships of pyrazine-2-carboxamide derivatives as novel echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase (ALK) inhibitors》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Iikubo, Kazuhiko; Kurosawa, Kazuo; Matsuya, Takahiro; Kondoh, Yutaka; Kamikawa, Akio; Moritomo, Ayako; Iwai, Yoshinori; Tomiyama, Hiroshi; Shimada, Itsuro. The article conveys some information:

Echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase (ALK) is a valid therapeutic target for the treatment of EML4-ALK-pos. non-small cell lung cancer (NSCLC). We discovered 12c as a novel and potent EML4-ALK inhibitor through structural optimization of 5a. In mice xenografted with 3T3 cells expressing EML4-ALK, oral administration of 12c demonstrated potent antitumor activity. This article describes the synthesis and biol. evaluation of pyrazine-2-carboxamide derivatives along with studies of their structure-activity relationship (SAR) using computational modeling. The experimental part of the paper was very detailed, including the reaction process of trans-4-Aminocyclohexanol(cas: 27489-62-9Application of 27489-62-9)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Many important products require amines as part of their syntheses. Methylamine is utilized in the production of the analgesic meperidine (trade name Demerol) and the photographic developer Metol (trademark), and dimethylamine is used in the synthesis of the antihistamine diphenhydramine (trade name Benadryl), the solvent dimethylformamide (DMF), and the rocket propellant 1,1-dimethylhydrazine. The synthesis of the insect repellent N,N-diethyl-m-toluamide (DEET) incorporates diethylamine while that of the synthetic fibre Kevlar requires aromatic amines.Application of 27489-62-9

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Category: alcohols-buliding-blocksIn 2020 ,《Sulfone-Mediated SNAr Reaction as a Powerful Tool for the Synthesis of 4-Quinolinyl Ethers and More-Application to the Synthesis of HCV NS3/4a Protease Inhibitor BI 201420》 appeared in Journal of Organic Chemistry. The author of the article were Patel, Nitinchandra D.; Wei, Xudong; Byrne, Denis; Narayanan, Bikshandarkoil A.; Pennino, Scott; Sarvestani, Max; Saha, Anjan; Haddad, Nizar; Kapadia, Suresh; Lorenz, Jon C.; DeCroos, Philomen; Ye, Andrew; Lee, Heewon; Grinberg, Nelu; Hossain, Azad; Busacca, Carl A.; Yee, Nathan K.; Senanayake, Chris H.. The article conveys some information:

4-Sulfonylquinolines and a 4-sulfonylpyridine underwent chemoselective nucleophilic aromatic substitution reactions with alcs. using either potassium tert-butoxide or potassium hexamethyldisilazide (when tertiary alcs. were used) in DMF to yield quinolinyl or pyridinyl ethers. Using this method, quinolinyl ether-containing HCV NS3/4a protease inhibitors BI 201420MU, BILN2061, and a related macrocyclic HCV protease inhibitor were prepared convergently. After reading the article, we found that the author used trans-4-Aminocyclohexanol(cas: 27489-62-9Category: alcohols-buliding-blocks)

trans-4-Aminocyclohexanol(cas: 27489-62-9) 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.Category: alcohols-buliding-blocks

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Name: trans-4-AminocyclohexanolIn 2021 ,《Discovery of Sisunatovir (RV521), an Inhibitor of Respiratory Syncytial Virus Fusion》 was published in Journal of Medicinal Chemistry. The article was written by Cockerill, G. Stuart; Angell, Richard M.; Bedernjak, Alexandre; Chuckowree, Irina; Fraser, Ian; Gascon-Simorte, Jose; Gilman, Morgan S. A.; Good, James A. D.; Harland, Rachel; Johnson, Sara M.; Ludes-Meyers, John H.; Littler, Edward; Lumley, James; Lunn, Graham; Mathews, Neil; McLellan, Jason S.; Paradowski, Michael; Peeples, Mark E.; Scott, Claire; Tait, Dereck; Taylor, Geraldine; Thom, Michelle; Thomas, Elaine; Villalonga Barber, Carol; Ward, Simon E.; Watterson, Daniel; Williams, Gareth; Young, Paul; Powell, Kenneth. The article contains the following contents:

RV521 is an orally bioavailable inhibitor of respiratory syncytial virus (RSV) fusion that was identified after a lead optimization process based upon hits that originated from a phys. property directed hit profiling exercise at Reviral. This exercise encompassed collaborations with a number of contract organizations with collaborative medicinal chem. and virol. during the optimization phase in addition to those utilized as the compound proceeded through preclin. and clin. evaluation. RV521 exhibited a mean IC50 of 1.2 nM against a panel of RSV A and B laboratory strains and clin. isolates with antiviral efficacy in the Balb/C mouse model of RSV infection. Oral bioavailability in preclin. species ranged from 42 to >100% with evidence of highly efficient penetration into lung tissue. In healthy adult human volunteers exptl. infected with RSV, a potent antiviral effect was observed with a significant reduction in viral load and symptoms compared to placebo. In addition to this study using trans-4-Aminocyclohexanol, there are many other studies that have used trans-4-Aminocyclohexanol(cas: 27489-62-9Name: trans-4-Aminocyclohexanol) was used in this study.

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. The reaction of alkyl halides, R―X, where X is a halogen, or analogous reagents with ammonia (or amines) is useful with certain compounds. Not all alkyl halides are effective reagents; the reaction is sluggish with secondary alkyl groups and fails with tertiary ones. Its usefulness is largely confined to primary alkyl halides (those having two hydrogen atoms on the reacting site).Name: trans-4-Aminocyclohexanol

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In 2018,Journal of Medicinal Chemistry included an article by Degorce, Sebastien L.; Bodnarchuk, Michael S.; Cumming, Iain A.; Scott, James S.. Recommanded Product: 27489-62-9. The article was titled 《Lowering Lipophilicity by Adding Carbon: One-Carbon Bridges of Morpholines and Piperazines》. The information in the text is summarized as follows:

In this article, we report our investigation of a phenomenon by which bridging morpholines across the ring with one-carbon tethers leads to a counterintuitive reduction in lipophilicity. This effect was also found to occur in piperazines and piperidines and lowered the measured log D7.4 of the bridged mols. by as much as -0.8 relative to their unbridged counterparts. As lowering lipophilicity without introducing addnl. heteroatoms can be desirable, we believe this potentially provides a useful tactic to improve the drug-like properties of mols. containing morpholine-, piperazine-, and piperidine-like motifs. The experimental part of the paper was very detailed, including the reaction process of trans-4-Aminocyclohexanol(cas: 27489-62-9Recommanded Product: 27489-62-9)

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Reaction with nitrous acid (HNO2), which functions as an acylating agent that is a source of the nitrosyl group (―NO), converts aliphatic primary amines to nitrogen and mixtures of alkenes and alcohols corresponding to the alkyl group in a complex process. This reaction has been used for analytical determination of primary amino groups in a procedure known as the Van Slyke method.Recommanded Product: 27489-62-9

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In 2018,de Velasco, Diego Antonio Ocampo Gutierrez; Su, Aoze; Zhai, Luhan; Kinoshita, Satowa; Otani, Yuko; Ohwada, Tomohiko published 《Unexpected resistance to base-catalyzed hydrolysis of nitrogen pyramidal amides based on the 7-azabicyclic[2.2.1]heptane scaffold》.Molecules published the findings.COA of Formula: C6H13NO The information in the text is summarized as follows:

Non-planar amides are usually transitional structures, that are involved in amide bond rotation and inversion of the nitrogen atom, but some ground-min. non-planar amides have been reported. Non-planar amides are generally sensitive to water or other nucleophiles, so that the amide bond is readily cleaved. In this article, examine the reactivity profile of the base-catalyzed hydrolysis of 7-azabicyclo[2.2.1]heptane amides I (R = H, Cl, NO2), which show pyramidalization of the amide nitrogen atom, and we compare the kinetics of the base-catalyzed hydrolysis of the benzamides of 7-azabicyclo[2.2.1]heptane and related monocyclic compounds Unexpectedly, non-planar amides based on the 7-azabicyclo[2.2.1]heptane scaffold were found to be resistant to base-catalyzed hydrolysis. The calculated Gibbs free energies were consistent with this exptl. finding. The contribution of thermal corrections (entropy term, -TΔS†) was large; the entropy term (ΔS†) took a large neg. value, indicating significant order in the transition structure, which includes solvating water mols. In addition to this study using trans-4-Aminocyclohexanol, there are many other studies that have used trans-4-Aminocyclohexanol(cas: 27489-62-9COA of Formula: C6H13NO) was used in this study.

trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Left-handed and right-handed forms (mirror-image configurations, known as optical isomers or enantiomers) are possible when all the substituents on the central nitrogen atom are different (i.e., the nitrogen is chiral). With amines, there is extremely rapid inversion in which the two configurations are interconverted.COA of Formula: C6H13NO

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