Category: 89466-08-0

In 2022,Ding, Yi-Xuan; Zhu, Zhou-Hao; Chen, Mu-Wang; Yu, Chang-Bin; Zhou, Yong-Gui published an article in Angewandte Chemie, International Edition. The title of the article was 《Rhodium-Catalyzed Asymmetric Hydrogenation of All-Carbon Aromatic Rings》.Recommanded Product: 89466-08-0 The author mentioned the following in the article:

Compared with heteroarenes, homogeneous asym. hydrogenation of all-carbon aromatic rings is a longstanding challenge in organic synthesis due to the strong aromaticity and difficult enantioselective control. Herein, authors report the rhodium/diphosphine-catalyzed asym. hydrogenation of all-carbon aromatic rings, affording a series of axially chiral cyclic compounds with high enantioselectivity through desymmetrization or kinetic resolution In addition, the central-chiral cyclic compounds were also obtained by asym. hydrogenation of phenanthrenes bearing a directing group. The key to success is the introduction of chiral diphosphine ligands with steric hindrance and strong electron-donating properties. The axially chiral monophosphine ligands could be obtained by simple conversion of the hydrogenation products bearing the phosphine atom. The experimental process involved the reaction of 2-Hydroxyphenylboronic acid(cas: 89466-08-0Recommanded Product: 89466-08-0)

2-Hydroxyphenylboronic acid(cas: 89466-08-0) belongs to acyl phenylboronic acid. Phenylboronic acid (PBA) has been used to extract β-blockers (a class of aminoalcohol-containing drugs) from aqueous solution, rat, and human plasma. Recommanded Product: 89466-08-0

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

《Alkyne Linchpin Strategy for Drug:Pharmacophore Conjugation: Experimental and Computational Realization of a Meta-Selective Inverse Sonogashira Coupling》 was written by Porey, Sandip; Zhang, Xinglong; Bhowmick, Suman; Kumar Singh, Vikas; Guin, Srimanta; Paton, Robert S.; Maiti, Debabrata. Product Details of 89466-08-0 And the article was included in Journal of the American Chemical Society in 2020. The article conveys some information:

The late-stage functionalization (LSF) of pharmaceutical and agrochem. compounds by the site-selective activation of C-H bonds provides access to diverse structural analogs and expands synthetically-accessible chem. space. We report a C-H functionalization LSF strategy that hinges on the use of an alkyne linchpin to assemble conjugates of sp2-rich marketed pharmaceuticals and agrochems. with sp3-rich 3D fragments and natural products. This is accomplished through a template-assisted inverse Sonogashira reaction that displays high levels of selectivity for the meta position. This protocol is also amenable to distal structural modifications of α-amino acids. The transformation of alkyne functionality to other functional groups further highlights the applicative potential. Computational and exptl. mechanistic studies shed light on the detailed mechanism. Turnover-limiting 1,2-migratory insertion of the bromoalkyne coupling partner occurs after relatively fast C-H activation. While this insertion occurs unselectively, regioconvergence results from one of the adducts undergoing a 1,2-trialkylsilyl migration to form the alkynylated product. A heterobimetallic Pd-Ag transition structure is essential for product formation in the β-bromide elimination step.2-Hydroxyphenylboronic acid(cas: 89466-08-0Product Details of 89466-08-0) was used in this study.

2-Hydroxyphenylboronic acid(cas: 89466-08-0) belongs to acyl phenylboronic acid. Phenylboronic acid (PBA) has been used to extract β-blockers (a class of aminoalcohol-containing drugs) from aqueous solution, rat, and human plasma. Product Details of 89466-08-0

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

《Hit-to-lead optimization of a latency-associated nuclear antigen inhibitor against Kaposi’s sarcoma-associated herpesvirus infections》 was written by Kirsch, Philine; Stein, Saskia C.; Berwanger, Aylin; Rinkes, Julia; Jakob, Valentin; Schulz, Thomas F.; Empting, Martin. Recommanded Product: 2-Hydroxyphenylboronic acid And the article was included in European Journal of Medicinal Chemistry in 2020. The article conveys some information:

The Latency-associated nuclear antigen (LANA) plays a central role for the latent persistence of the Kaposi’s Sarcoma Herpesvirus (KSHV) in the human host and helps to establish lifelong infections. Herein, we report our efforts towards hit-to-lead generation starting from a previously discovered LANA-DNA inhibitor. By tethering the viral genome to the host nucleosomes, LANA ensures the segregation and persistence of the viral DNA during mitosis. LANA is also required for the replication of the latent viral episome during the S phase of the cell cycle. We aim to inhibit the interaction between LANA and the viral genome to prevent the latent persistence of KSHV in the host organism. Medicinal chem.-driven optimization studies and structure-activity-relationship investigation led to the discovery of an improved LANA inhibitor. The functional activity of our compounds was evaluated using a fluorescence polarization (FP)-based interaction inhibition assay and electrophoretic mobility shift assay (EMSA). Even though a crystal structure of the ligand protein complex was not available, we successfully conducted hit optimization toward a low micromolar protein-nucleic acid-interaction inhibitor. Addnl., we applied STD-NMR studies to corroborate target binding and to gain insights into the binding orientation of our most potent inhibitor, providing opportunities for further rational design of more efficient LANA-targeting anti KSHV agents in future studies. After reading the article, we found that the author used 2-Hydroxyphenylboronic acid(cas: 89466-08-0Recommanded Product: 2-Hydroxyphenylboronic acid)

2-Hydroxyphenylboronic acid(cas: 89466-08-0) belongs to acyl phenylboronic acid. Phenylboronic acid (PBA) has been used to extract β-blockers (a class of aminoalcohol-containing drugs) from aqueous solution, rat, and human plasma. Recommanded Product: 2-Hydroxyphenylboronic acid

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Product Details of 89466-08-0In 2021 ,《Design, synthesis and pharmacological evaluation of bicyclic and tetracyclic pyridopyrimidinone analogs as new KRASG12C inhibitors》 was published in European Journal of Medicinal Chemistry. The article was written by Xiao, Xuanzheng; Lai, Mengzhen; Song, Zilan; Geng, Meiyu; Ding, Jian; Xie, Hua; Zhang, Ao. The article contains the following contents:

KRAS is the most commonly altered oncogene of the RAS family, especially the G12C mutant (KRASG12C), which has been a promising drug target for many cancers. On the basis of the bicyclic pyridopyrimidinone framework of the first-in-class clin. KRASG12C inhibitor AMG510, a scaffold hopping strategy was conducted including a F-OH cyclization approach and a pyridinyl N-atom working approach leading to new tetracyclic and bicyclic analogs. Compound (I) was identified possessing binding potency of 1.87μM against KRASG12C and cell growth inhibition of 0.79μM in MIA PaCa-2 pancreatic cancer cells. Treatment of I with NCI-H358 cells resulted in down-regulation of KRAS-GTP levels and reduction of phosphorylation of downstream ERK and AKT dose-dependently. Mol. docking suggested that the fluorophenol moiety of I occupies a hydrophobic pocket region thus forming hydrogen bonding to Arg68. These results will be useful to guide further structural modification.2-Hydroxyphenylboronic acid(cas: 89466-08-0Product Details of 89466-08-0) was used in this study.

2-Hydroxyphenylboronic acid(cas: 89466-08-0) belongs to acyl phenylboronic acid. Phenylboronic acid (PBA), a synthetic molecule applied in RNA affinity chromatography, is able to form reversible covalent ester bonds with 1,2- or 1,3-cis-doils on the ribose ringProduct Details of 89466-08-0

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Alcohol – Wikipedia,
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Quality Control of 2-Hydroxyphenylboronic acidIn 2021 ,《Design and synthesis of 1H-pyrazolo[3,4-b]pyridines targeting mitogen-activated protein kinase kinase 4 (MKK4) – A promising target for liver regeneration》 appeared in European Journal of Medicinal Chemistry. The author of the article were Pfaffenrot, Bent; Kloevekorn, Philip; Juchum, Michael; Selig, Roland; Albrecht, Wolfgang; Zender, Lars; Laufer, Stefan A.. The article conveys some information:

Currently, the therapeutic options for treatment of liver failure are very limited. As mitogen-activated protein kinase kinase 4 (MKK4) has recently been identified by in vivo RNAi experiments to be a major regulator in hepatocyte regeneration, authors pursued the development of a small mol. targeting this protein kinase. Starting from the approved BRAFV600E inhibitor vemurafenib, that showed a high off-target affinity to MKK4 in an initial screening, authors followed a scaffold-hopping approach, changing the core heterocycle from 1H-pyrrolo[2,3-b]pyridine to 1H-pyrazolo[2,3-b]pyridine I. Affinity to MKK4 could be conserved while the selectivity against off-target protein kinases was slightly improved. Further modifications led to II and III showing high affinity to MKK4 in the low nanomolar range and excellent selectivity profile from mandatory multiparameter-optimization for the essential anti-targets (MKK7, JNK1) and off-targets (BRAF, MAP4K5, ZAK) in the MKK4 pathway. Herein authors report the first selective MKK4 inhibitors in this class. In the part of experimental materials, we found many familiar compounds, such as 2-Hydroxyphenylboronic acid(cas: 89466-08-0Quality Control of 2-Hydroxyphenylboronic acid)

2-Hydroxyphenylboronic acid(cas: 89466-08-0) belongs to acyl phenylboronic acid. Phenylboronic acid (PBA) has been used to extract β-blockers (a class of aminoalcohol-containing drugs) from aqueous solution, rat, and human plasma. Quality Control of 2-Hydroxyphenylboronic acid

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In 2019,European Journal of Inorganic Chemistry included an article by Buchner, Magnus R.; Mueller, Matthias; Raymond, Onyekachi; Severinsen, Rebecca J.; Nixon, David J.; Henderson, William; Brothers, Penelope J.; Rowlands, Gareth J.; Plieger, Paul G.. COA of Formula: C6H7BO3. The article was titled 《Synthesis of a Boronic Acid Anhydride Based Ligand and Its Application in Beryllium Coordination》. The information in the text is summarized as follows:

The synthesis of a boronic acid anhydride-based ligand containing one three- and one four-coordinated B atom is presented. This ligand was successfully employed as a tridentate κ1N,κ2O-ligand in the coordination of Be chloride and both the ligand and the resulting complex were structurally characterized. While the B-element separations are within the typical range of related homo-nuclear compounds, the corresponding Be-element distances are rather long, suggesting unexpectedly high electron d. at the Be center. Incorporation of a Be atom in a six-membered ring causes no more distortion than the corresponding B atom, suggesting that analogous ligand systems could be used in B and Be coordination chem. The generated hetero-tri-nuclear complex enables the direct comparison of bond lengths and angles at Be and B atoms in similar coordination environments and can act as a monomol. model for Be borates. In the part of experimental materials, we found many familiar compounds, such as 2-Hydroxyphenylboronic acid(cas: 89466-08-0COA of Formula: C6H7BO3)

2-Hydroxyphenylboronic acid(cas: 89466-08-0) belongs to acyl phenylboronic acid. Phenylboronic acid (PBA) has been used to extract β-blockers (a class of aminoalcohol-containing drugs) from aqueous solution, rat, and human plasma. COA of Formula: C6H7BO3

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

《Rational computational design of fourth-generation EGFR inhibitors to combat drug-resistant non-small cell lung cancer》 was written by Park, Hwangseo; Jung, Hoi-Yun; Kim, Kewon; Kim, Myojeong; Hong, Sungwoo. Product Details of 89466-08-0 And the article was included in International Journal of Molecular Sciences in 2020. The article conveys some information:

Herein, we report the discovery of potent and highly selective inhibitors of EGFR exon 19 p.E746_A750del/EGFR exon 20 p.T790M/EGFR exon 20 p.C797S (d746-750/T790M/C797S) mutant, which were derived via two-track virtual screening and de novo design. This two-track approach was performed so as to maximize and minimize the inhibitory activity against the triple mutant and the wild type, resp. Extensive chem. modifications of the initial hit compounds led to the identification of several low-nanomolar inhibitors of the d746-750/T790M/C797S mutant. The formations of a hydrogen bond with the mutated residue Ser797 and the van der Waals contact with the mutated residue Met790 were found to be a common feature in the interactions between EGFRd746-750/T790M/C797S and the fourth-generation inhibitors. Such an exceptionally high selectivity could also be attributed to the formation of the hydrophobic contact with a Gly loop residue or the hydrogen bond with Asp855 in the activation loop. The discovery of the potent and selective EGFRd746-750/T790M/C797S inhibitors were actually made possible by virtue of the modified protein-ligand binding free energy function involving a new hydration free energy term with enhanced accuracy. The fourth-generation EGFR inhibitors found in this work are anticipated to serve as a new starting point for the discovery of anti-NSCLC medicines to overcome the problematic drug resistance. After reading the article, we found that the author used 2-Hydroxyphenylboronic acid(cas: 89466-08-0Product Details of 89466-08-0)

2-Hydroxyphenylboronic acid(cas: 89466-08-0) belongs to acyl phenylboronic acid. Phenylboronic acid (PBA) has been used to extract β-blockers (a class of aminoalcohol-containing drugs) from aqueous solution, rat, and human plasma. Product Details of 89466-08-0

Referemce:
Alcohol – Wikipedia,
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In 2022,Plaza-Pedroche, Rodrigo; Fernandez-Liencres, M. Paz; Jimenez-Pulido, Sonia B.; Illan-Cabeza, Nuria A.; Achelle, Sylvain; Navarro, Amparo; Rodriguez-Lopez, Julian published an article in ACS Applied Materials & Interfaces. The title of the article was 《Excited-State Intramolecular Proton Transfer in 2-(2′-Hydroxyphenyl)pyrimidines: Synthesis, Optical Properties, and Theoretical Studies》.Safety of 2-Hydroxyphenylboronic acid The author mentioned the following in the article:

The development of fluorescence materials with switched on/off emission has attracted great attention owing to the potential application of these materials in chem. sensing. In this work, the photophys. properties of a series of original 2-(2′-hydroxyphenyl)pyrimidines were thoroughly studied. The compounds were prepared by following well-established and straightforward methodologies and showed very little or null photoluminescence both in solution and in the solid state. This absence of emission can be explained by a fast proton transfer from the OH group to the nitrogen atoms of the pyrimidine ring to yield an excited tautomer that deactivates through a nonradiative pathway. The key role of the OH group in the emission quenching was demonstrated by the preparation of 2′-unsubstituted derivatives, all of which exhibited violet or blue luminescence. Single crystals of some compounds suitable for an X-ray diffraction anal. could be obtained, which permitted us to investigate inter- and intramol. interactions and mol. packing structures. The protonation of the pyrimidine ring by an addition of trifluoroacetic acid inhibited the excited-state intramol. proton transfer (ESIPT) process, causing a reversible switch on fluorescence response detectable by the naked eye. This acidochromic behavior allows 2-(2′-hydroxyphenyl)pyrimidines to be used as solid-state acid-base vapor sensors and anticounterfeiting agents. Extensive d. functional theory and its time-dependent counterpart calculations at the M06-2X/6-31+G** level of theory were performed to rationalize all the exptl. results and understand the impact of protonation on the different optical transitions. In the experiment, the researchers used many compounds, for example, 2-Hydroxyphenylboronic acid(cas: 89466-08-0Safety of 2-Hydroxyphenylboronic acid)

2-Hydroxyphenylboronic acid(cas: 89466-08-0) belongs to acyl phenylboronic acid. Phenylboronic acid (PBA) has been used to extract β-blockers (a class of aminoalcohol-containing drugs) from aqueous solution, rat, and human plasma. Safety of 2-Hydroxyphenylboronic acid

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Synthetic Route of C6H7BO3In 2021 ,《Synthesis of Pyrroles via Consecutive 6π-Electrocyclization/Ring-Contraction of Sulfilimines》 appeared in Journal of the American Chemical Society. The author of the article were Haut, Franz-Lucas; Feichtinger, Niklas J.; Plangger, Immanuel; Wein, Lukas A.; Mueller, Mira; Streit, Tim-Niclas; Wurst, Klaus; Podewitz, Maren; Magauer, Thomas. The article conveys some information:

Authors present a modular, synthetic entry to polysubstituted pyrroles employing readily available 2,5-dihydrothiophenes. Ring-opening of the heterocycle provides access to a panel of 1,3-dienes which underwent pyrrole formation in the presence of inexpensive chloramine-T trihydrate. The transformation is conducted in an open flask and proceeds at ambient temperatures (23°) in nondry solvents. A careful adjustment of the electronics and sterics of the 1,3-diene precursor allows for the isolation of key intermediates. DFT studies identified a reaction mechanism that features a 6π-electrocyclization of a sulfilimine intermediate followed by spontaneous ring-contraction to reveal the pyrrole skeleton. In the part of experimental materials, we found many familiar compounds, such as 2-Hydroxyphenylboronic acid(cas: 89466-08-0Synthetic Route of C6H7BO3)

2-Hydroxyphenylboronic acid(cas: 89466-08-0) belongs to acyl phenylboronic acid. Phenylboronic acid (PBA) has been used to extract β-blockers (a class of aminoalcohol-containing drugs) from aqueous solution, rat, and human plasma. Synthetic Route of C6H7BO3

Referemce:
Alcohol – Wikipedia,
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Product Details of 89466-08-0In 2019 ,《Palladium-Catalyzed Directed meta-Selective C-H Allylation of Arenes: Unactivated Internal Olefins as Allyl Surrogates》 appeared in Angewandte Chemie, International Edition. The author of the article were Achar, Tapas Kumar; Zhang, Xinglong; Mondal, Rahul; Shanavas, M. S.; Maiti, Siddhartha; Maity, Sabyasachi; Pal, Nityananda; Paton, Robert S.; Maiti, Debabrata. The article conveys some information:

Palladium(II)-catalyzed meta-selective C-H allylation of arenes RC6H4(CH2)nXR1 [R = H, 3-Me, 3-Br, 4-F, etc.; R1 = 2-(pyrimidin-5-yl)phenoxy, 2-(pyridin-3-yl)phenoxy, 2-(8-nitroquinolin-3-yl)phenoxy, etc.; X = SO2, C(O), Si(i-Pr)2, CH2; n = 1-4] including 2-(pyrimidin-5-yl)phenyl (2S)-2-(6-methoxynaphthalen-2-yl)propanoate has been developed utilizing synthetically inert unactivated acyclic internal olefins R2CH2CH=CHCH2R3 [R2 = Me, Et, n-Pr, pentyl, etc.; R3 = Me, COOMe, [[(1S,2R,5S)-5-methyl-2-(propan-2-yl)cyclohexyl]oxy]carbonyl, etc.] as allylic surrogates. The strong σ-donating and π-accepting ability of pyrimidine-based directing group facilitates the olefin insertion by overcoming inertness of the typical unactivated internal olefins. Exclusive allyl over styrenyl products, e.g., (E)-I selectivity as well as E stereoselectivity were achieved with broad substrate scope, wide functional-group tolerance, and good to excellent yields. Late-stage functionalizations of pharmaceuticals were demonstrated. Exptl. and computational studies shed light on the mechanism and point to key steric control in the palladacycle, thus determining product selectivities. The experimental process involved the reaction of 2-Hydroxyphenylboronic acid(cas: 89466-08-0Product Details of 89466-08-0)

2-Hydroxyphenylboronic acid(cas: 89466-08-0) belongs to acyl phenylboronic acid. Phenylboronic acid (PBA) has been used to extract β-blockers (a class of aminoalcohol-containing drugs) from aqueous solution, rat, and human plasma. Product Details of 89466-08-0

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts