Tag: M.W=150-200

Some low molecular weight alcohols of industrial importance are produced by the addition of water to alkenes. 72824-04-5, formula is C9H17BO2, Ethanol, isopropanol, 2-butanol, and tert-butanol are produced by this general method. Two implementations are employed, the direct and indirect methods. Electric Literature of 72824-04-5

Michalland, Jean;Casaretto, Nicolas;Zard, Samir Z. research published 《 A Modular Access to 1,2- and 1,3-Disubstituted Cyclobutylboronic Esters by Consecutive Radical Additions》, the research content is summarized as follows. A modular approach to substituted cyclobutylboronic esters is described. It proceeds by successive intermol. radical additions of xanthates to pinacolato 1-cyclobutenylboronate and to pinacolato bicyclo[1.1.0]but-1-ylboronate. Success hinges on tuning the stability of the α-boryl radical by exploiting the stabilizing influence of the trivalent boronic ester and the slightly destabilizing cyclobutane, which increases the σ-character of the radical. Reductive removal of the xanthate group finally provides a range of 1,2- and 1,3-disubstituted cyclobutylboronic esters. The contrast with cyclopropylboronic esters is striking, since the strong destabilization by the highly strained cyclopropane ring allows the first radical addition to take place but not the second. Furthermore, the first adducts are geminal xanthyl boronic esters that can be converted into cyclobutanones. This chem. furnishes cyclobutylboronic esters that would be quite difficult to obtain otherwise and thus complements existing methods.

72824-04-5, Allylboronic acid pinacol ester is a useful research compound. Its molecular formula is C9H17BO2 and its molecular weight is 168.04 g/mol. The purity is usually 95%.
Allylboronic acid pinacol ester is an allylation reagent that is used to produce aldehydes from ketones. It reacts with water, yielding the desired product and formaldehyde as a byproduct. The reaction proceeds through a sequence of steps, in which the boronate ester first reacts with water to form an allylboronate ion and hydrogen gas. This intermediate then reacts with potassium t-butoxide to produce the desired allyl alcohol and potassium borohydride. Finally, the palladium complex catalyst reduces the carbonyl group of the starting material, converting it into an aldehyde. Allylboronic acid pinacol ester is commercially available as a white solid, but can also be synthesized from 2-chloro-5-pinacolylborane (pinacol) in high yield using catalytic cross coupling reactions., Electric Literature of 72824-04-5

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Simple alcohols are found widely in nature. Ethanol is the most prominent because it is the product of fermentation, a major energy-producing pathway. 141699-55-0, formula is C8H15NO3, Other simple alcohols, chiefly fusel alcohols, are formed in only trace amounts. More complex alcohols however are pervasive, as manifested in sugars, some amino acids, and fatty acids. , Recommanded Product: tert-Butyl 3-hydroxyazetidine-1-carboxylate

Mikus, Malte S.;Sanchez, Carina;Fridrich, Cary;Larrow, Jay F. research published 《 Palladium Catalyzed C-O Coupling of Amino Alcohols for the Synthesis of Aryl Ethers》, the research content is summarized as follows. Amine containing aryl ethers are common pharmacophore motifs that continue to emerge from drug discovery efforts. As amino alcs. are readily available building blocks, practical methodologies for incorporating them into more complex structures are highly desirable. We report our efforts to explore the application of Pd-catalyzed C-O coupling methods to the arylation of 1,2- and 1,3-amino alcs. [e.g., 1-bromo-4-(trifluoromethyl)benzene + amino alc. I → II (82%, 68% isolated)]. We established general and reliable conditions, under which we explored the scope and limitations of the transformation. The insights gained have been valuable in employing this methodol. within a fast-moving drug discovery environment, which we anticipate will be of general interest to the synthesis and catalysis communities.

Recommanded Product: tert-Butyl 3-hydroxyazetidine-1-carboxylate, Tert-butyl 3-hydroxyazetidine-1-carboxylate is a useful research compound. Its molecular formula is C8H15NO3 and its molecular weight is 173.21 g/mol. The purity is usually 95%.

Tert-butyl 3-hydroxyazetidine-1-carboxylate has been shown to be a good substrate for the preparation of N-protected amino alcohols and amines by the process of reductive amination. In this synthesis, tert-butyl azetidinium chloride is used as a catalyst in the reaction with sodium hydroxide. The tert-butyl group can be removed using ammonium hydroxide in the presence of a base such as triethylamine. This reaction can be performed on a large scale, making it useful in the manufacture of pharmaceuticals. The efficiency and solubility of this process make it suitable for use as an introduction to other processes involving N-protected amino alcohols or amines., 141699-55-0.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Simple alcohols are found widely in nature. Ethanol is the most prominent because it is the product of fermentation, a major energy-producing pathway. 72824-04-5, formula is C9H17BO2, Other simple alcohols, chiefly fusel alcohols, are formed in only trace amounts. More complex alcohols however are pervasive, as manifested in sugars, some amino acids, and fatty acids. , Electric Literature of 72824-04-5

Miura, Hiroki;Hachiya, Yuka;Nishio, Hidenori;Fukuta, Yohei;Toyomasu, Tomoya;Kobayashi, Kosa;Masaki, Yosuke;Shishido, Tetsuya research published 《 Practical Synthesis of Allyl, Allenyl, and Benzyl Boronates through S_N1′-Type Borylation under Heterogeneous Gold Catalysis》, the research content is summarized as follows. Efficient borylation of sp3 C-O bonds by supported Au catalysts is described. Au nanoparticles supported on TiO2 showed high activity under mild conditions employing low catalyst loading conditions without the aid of any additives, such as phosphine and bases. A variety of allyl, propargyl, and benzyl substrates participated in the heterogeneously catalyzed reactions to furnish the corresponding allyl, allenyl, and benzyl boronates in high yields. Besides, Au/TiO2 was also effective for the direct borylation of allylic and benzylic alcs. A mechanistic investigation based on a Hammett study and control experiments revealed that sp3 C-O bond borylation over supported Au catalysts proceeded through SN1′-type mechanism involving the formation of a carbocationic intermediate. The high activity, reusability, and environmental compatibility of the supported Au catalysts as well as the scalability of the reaction system enable the practical synthesis of valuable organoboron compounds

Electric Literature of 72824-04-5, Allylboronic acid pinacol ester is a useful research compound. Its molecular formula is C9H17BO2 and its molecular weight is 168.04 g/mol. The purity is usually 95%.
Allylboronic acid pinacol ester is an allylation reagent that is used to produce aldehydes from ketones. It reacts with water, yielding the desired product and formaldehyde as a byproduct. The reaction proceeds through a sequence of steps, in which the boronate ester first reacts with water to form an allylboronate ion and hydrogen gas. This intermediate then reacts with potassium t-butoxide to produce the desired allyl alcohol and potassium borohydride. Finally, the palladium complex catalyst reduces the carbonyl group of the starting material, converting it into an aldehyde. Allylboronic acid pinacol ester is commercially available as a white solid, but can also be synthesized from 2-chloro-5-pinacolylborane (pinacol) in high yield using catalytic cross coupling reactions., 72824-04-5.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

With respect to acute toxicity, simple alcohols have low acute toxicities. Doses of several milliliters are tolerated. 72824-04-5, formula is C9H17BO2, For pentanols, hexanols, octanols and longer alcohols, LD50 range from 2–5 g/kg (rats, oral). Ethanol is less acutely toxic.All alcohols are mild skin irritants. Recommanded Product: 2-Allyl-4,4,5,5-tetramethyl-1,3,2-dioxaborolane

Morrison, Ryan J.;van der Mei, Farid W.;Romiti, Filippo;Hoveyda, Amir H. research published 《 A Catalytic Approach for Enantioselective Synthesis of Homoallylic Alcohols Bearing a Z-Alkenyl Chloride or Trifluoromethyl Group. A Concise and Protecting Group-Free Synthesis of Mycothiazole》, the research content is summarized as follows. A protecting group-free strategy is presented for diastereo- and enantioselective routes that can be used to prepare a wide variety of Z-homoallylic alcs. with significantly higher efficiency than is otherwise feasible. The approach entails the merger of several catalytic processes and is expected to facilitate the preparation of bioactive organic mols. More specifically, Z-chloro-substituted allylic pinacolatoboronate is first obtained through stereoretentive cross-metathesis between Z-crotyl-B(pin) (pin = pinacolato) and Z-dichloroethene, both of which are com. available. The organoboron compound may be used in the central transformation of the entire approach, an α- and enantioselective addition to an aldehyde, catalyzed by a proton-activated, chiral aminophenol-boryl catalyst. Catalytic cross-coupling can then furnish the desired Z-homoallylic alc. in high enantiomeric purity. The olefin metathesis step can be carried out with substrates and a Mo-based complex that can be purchased. The aminophenol compound that is needed for the second catalytic step can be prepared in multigram quantities from inexpensive starting materials. A significant assortment of homoallylic alcs. bearing a Z-F₃C-substituted alkene can also be prepared with similar high efficiency and regio-, diastereo-, and enantioselectivity. What is more, trisubstituted Z-alkenyl chloride moiety can be accessed with similar efficiency albeit with somewhat lower α-selectivity and enantioselectivity. The general utility of the approach is underscored by a succinct, protecting group-free, and enantioselective total synthesis of mycothiazole, a naturally occurring anticancer agent through a sequence that contains a longest linear sequence of nine steps (12 steps total), seven of which are catalytic, generating mycothiazole in 14.5% overall yield.

Recommanded Product: 2-Allyl-4,4,5,5-tetramethyl-1,3,2-dioxaborolane, Allylboronic acid pinacol ester is a useful research compound. Its molecular formula is C9H17BO2 and its molecular weight is 168.04 g/mol. The purity is usually 95%.
Allylboronic acid pinacol ester is an allylation reagent that is used to produce aldehydes from ketones. It reacts with water, yielding the desired product and formaldehyde as a byproduct. The reaction proceeds through a sequence of steps, in which the boronate ester first reacts with water to form an allylboronate ion and hydrogen gas. This intermediate then reacts with potassium t-butoxide to produce the desired allyl alcohol and potassium borohydride. Finally, the palladium complex catalyst reduces the carbonyl group of the starting material, converting it into an aldehyde. Allylboronic acid pinacol ester is commercially available as a white solid, but can also be synthesized from 2-chloro-5-pinacolylborane (pinacol) in high yield using catalytic cross coupling reactions., 72824-04-5.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

With respect to acute toxicity, simple alcohols have low acute toxicities. Doses of several milliliters are tolerated. 72824-04-5, formula is C9H17BO2, For pentanols, hexanols, octanols and longer alcohols, LD50 range from 2–5 g/kg (rats, oral). Ethanol is less acutely toxic.All alcohols are mild skin irritants. Recommanded Product: 2-Allyl-4,4,5,5-tetramethyl-1,3,2-dioxaborolane

Lu, Yi;Sugita, Hajime;Mikami, Koichiro;Aoki, Daisuke;Otsuka, Hideyuki research published 《 Mechanochemical Reactions of Bis(9-methylphenyl-9-fluorenyl) Peroxides and Their Applications in Cross-Linked Polymers》, the research content is summarized as follows. The exploration of mechanochem. reactions has brought new opportunities for the design of functional materials. The authors synthesized the novel organic peroxide mechanophore bis(9-methylphenyl-9-fluorenyl) peroxide (BMPF) and examined its mechanochromic properties. The mechanism behind its mechanofluorescence was clarified and harnessed in polymer networks that can release the small fluorescent mol. 9-fluorenone upon exposure to a mech. stimulus. Addnl., polymer networks crosslinked with BMPF units are able to tolerate temperatures up to 110°C without any change in optical properties or mech. strength. As mechanophores based on organic peroxide have rarely been documented so far, these fascinating results suggest excellent potential for applications of BMPF in stress-responsive materials. The mechanochem. protocol demonstrated here may provide guiding principles to expand the field of mechanochromic peroxides.

Recommanded Product: 2-Allyl-4,4,5,5-tetramethyl-1,3,2-dioxaborolane, Allylboronic acid pinacol ester is a useful research compound. Its molecular formula is C9H17BO2 and its molecular weight is 168.04 g/mol. The purity is usually 95%.
Allylboronic acid pinacol ester is an allylation reagent that is used to produce aldehydes from ketones. It reacts with water, yielding the desired product and formaldehyde as a byproduct. The reaction proceeds through a sequence of steps, in which the boronate ester first reacts with water to form an allylboronate ion and hydrogen gas. This intermediate then reacts with potassium t-butoxide to produce the desired allyl alcohol and potassium borohydride. Finally, the palladium complex catalyst reduces the carbonyl group of the starting material, converting it into an aldehyde. Allylboronic acid pinacol ester is commercially available as a white solid, but can also be synthesized from 2-chloro-5-pinacolylborane (pinacol) in high yield using catalytic cross coupling reactions., 72824-04-5.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Simple alcohols are found widely in nature. Ethanol is the most prominent because it is the product of fermentation, a major energy-producing pathway. 72824-04-5, formula is C9H17BO2, Other simple alcohols, chiefly fusel alcohols, are formed in only trace amounts. More complex alcohols however are pervasive, as manifested in sugars, some amino acids, and fatty acids. , Electric Literature of 72824-04-5

Lv, Leiyang;Qian, Huijun;Crowell, Anna B.;Chen, Shuming;Li, Zhiping research published 《 Pd/NHC-Controlled Regiodivergent Defluorinative Allylation of gem-Difluorocyclopropanes with Allylboronates》, the research content is summarized as follows. Controlling the selectivity of synthetically useful reactions has been a longstanding objective of organic chem. Authors report a regiodivergent synthetic protocol allowing access to diverse fluorinated 1,5-dienes through Pd/NHC-catalyzed ring-opening allylation of gem-difluorocyclopropanes. D. functional theory (DFT) calculations on regioselectivity-determining transition states provided critical insight into the design of the NHC ligand for switching regioselectivity. Consistent with the DFT predictions, N-heterocyclic carbene (NHC) ligands with bulky ortho substituents favored branched allylation, with the IHept ligand providing > 20:1 branched/linear regioselectivity. NHC ligands with less hindered ortho substituents such as IMes favored the thermodynamically more stable linear products. Authors were able to carry out late-stage modification of various complex mols. using this protocol. Authors ligand-controlled approach provides efficient access to regioisomeric fluorinated 1,5-dienes from the same starting materials and constitutes a valuable addition to the toolbox of diversity-oriented synthesis.

72824-04-5, Allylboronic acid pinacol ester is a useful research compound. Its molecular formula is C9H17BO2 and its molecular weight is 168.04 g/mol. The purity is usually 95%.
Allylboronic acid pinacol ester is an allylation reagent that is used to produce aldehydes from ketones. It reacts with water, yielding the desired product and formaldehyde as a byproduct. The reaction proceeds through a sequence of steps, in which the boronate ester first reacts with water to form an allylboronate ion and hydrogen gas. This intermediate then reacts with potassium t-butoxide to produce the desired allyl alcohol and potassium borohydride. Finally, the palladium complex catalyst reduces the carbonyl group of the starting material, converting it into an aldehyde. Allylboronic acid pinacol ester is commercially available as a white solid, but can also be synthesized from 2-chloro-5-pinacolylborane (pinacol) in high yield using catalytic cross coupling reactions., Electric Literature of 72824-04-5

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Some low molecular weight alcohols of industrial importance are produced by the addition of water to alkenes. 141699-55-0, formula is C8H15NO3, Ethanol, isopropanol, 2-butanol, and tert-butanol are produced by this general method. Two implementations are employed, the direct and indirect methods. Product Details of C8H15NO3

Malamas, Michael S.;Farah, Shrouq I.;Lamani, Manjunath;Pelekoudas, Dimitrios N.;Perry, Nicholas Thomas;Rajarshi, Girija;Miyabe, Christina Yume;Chandrashekhar, Honrao;West, Jay;Pavlopoulos, Spiro;Makriyannis, Alexandros research published 《 Design and synthesis of cyanamides as potent and selective N-acylethanolamine acid amidase inhibitors》, the research content is summarized as follows. N-acylethanolamine acid amidase (NAAA) inhibition represents an exciting novel approach to treat inflammation and pain. NAAA is a cysteine amidase which preferentially hydrolyzes the endogenous biolipids palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). PEA is an endogenous agonist of the nuclear peroxisome proliferator-activated receptor-α (PPAR-α), which is a key regulator of inflammation and pain. Thus, blocking the degradation of PEA with NAAA inhibitors results in augmentation of the PEA/PPAR-α signaling pathway and regulation of inflammatory and pain processes. We have prepared a new series of NAAA inhibitors exploring the azetidine-nitrile (cyanamide) pharmacophore that led to the discovery of highly potent and selective compounds Key analogs demonstrated single-digit nanomolar potency for hNAAA and showed >100-fold selectivity against serine hydrolases FAAH, MGL and ABHD6, and cysteine protease cathepsin K. Addnl., we have identified potent and selective dual NAAA-FAAH inhibitors to investigate a potential synergism between two distinct anti-inflammatory mol. pathways, the PEA/PPAR-α anti-inflammatory signaling pathway,^1-4 and the cannabinoid receptors CB1 and CB2 pathways which are known for their antiinflammatory and antinociceptive properties.^5-8 Our ligand design strategy followed a traditional structure-activity relationship (SAR) approach and was supported by mol. modeling studies of reported X-ray structures of hNAAA. Several inhibitors were evaluated in stability assays and demonstrated very good plasma stability (t_1/2 > 2 h; human and rodents). The disclosed cyanamides represent promising new pharmacol. tools to investigate the potential role of NAAA inhibitors and dual NAAA-FAAH inhibitors as therapeutic agents for the treatment of inflammation and pain.

141699-55-0, Tert-butyl 3-hydroxyazetidine-1-carboxylate is a useful research compound. Its molecular formula is C8H15NO3 and its molecular weight is 173.21 g/mol. The purity is usually 95%.

Tert-butyl 3-hydroxyazetidine-1-carboxylate has been shown to be a good substrate for the preparation of N-protected amino alcohols and amines by the process of reductive amination. In this synthesis, tert-butyl azetidinium chloride is used as a catalyst in the reaction with sodium hydroxide. The tert-butyl group can be removed using ammonium hydroxide in the presence of a base such as triethylamine. This reaction can be performed on a large scale, making it useful in the manufacture of pharmaceuticals. The efficiency and solubility of this process make it suitable for use as an introduction to other processes involving N-protected amino alcohols or amines., Product Details of C8H15NO3

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In general, the hydroxyl group makes alcohols polar. Those groups can form hydrogen bonds to one another and to most other compounds. 141699-55-0, formula is C8H15NO3, Owing to the presence of the polar OH alcohols are more water-soluble than simple hydrocarbons. Methanol, ethanol, and propanol are miscible in water. Butanol, with a four-carbon chain, is moderately soluble. Recommanded Product: tert-Butyl 3-hydroxyazetidine-1-carboxylate

McDermott, Lee A.;Iyer, Prema;Vernetti, Larry;Rimer, Shawn;Sun, Jingran;Boby, Melissa;Yang, Tianyi;Fioravanti, Michael;O’Neill, Jason;Wang, Liwei;Drakes, Dylan;Katt, William;Huang, Qingqiu;Cerione, Richard research published 《 Design and evaluation of novel glutaminase inhibitors》, the research content is summarized as follows. A novel set of GAC (kidney glutaminase isoform C) inhibitors able to inhibit the enzymic activity of GAC and the growth of the triple neg. MDA-MB-231 breast cancer cells with low nanomolar potency is described. Compounds in this series have a reduced number of rotatable bonds, improved C log Ps, microsomal stability and ligand efficiency when compared to the leading GAC inhibitors BPTES and CB-839. Property improvements were achieved by the replacement of the flexible n-diethylthio or the Bu moiety present in the leading inhibitors by heteroatom substituted heterocycloalkanes.

Recommanded Product: tert-Butyl 3-hydroxyazetidine-1-carboxylate, Tert-butyl 3-hydroxyazetidine-1-carboxylate is a useful research compound. Its molecular formula is C8H15NO3 and its molecular weight is 173.21 g/mol. The purity is usually 95%.

Tert-butyl 3-hydroxyazetidine-1-carboxylate has been shown to be a good substrate for the preparation of N-protected amino alcohols and amines by the process of reductive amination. In this synthesis, tert-butyl azetidinium chloride is used as a catalyst in the reaction with sodium hydroxide. The tert-butyl group can be removed using ammonium hydroxide in the presence of a base such as triethylamine. This reaction can be performed on a large scale, making it useful in the manufacture of pharmaceuticals. The efficiency and solubility of this process make it suitable for use as an introduction to other processes involving N-protected amino alcohols or amines., 141699-55-0.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

With respect to acute toxicity, simple alcohols have low acute toxicities. Doses of several milliliters are tolerated. 141699-55-0, formula is C8H15NO3, For pentanols, hexanols, octanols and longer alcohols, LD50 range from 2–5 g/kg (rats, oral). Ethanol is less acutely toxic.All alcohols are mild skin irritants. Application In Synthesis of 141699-55-0

Liu, Yongfu;Wu, Jun;Zhou, Mingwei;Chen, Wenming;Li, Dongbo;Wang, Zhanguo;Hornsperger, Benoit;Aebi, Johannes D.;Marki, Hans-Peter;Kuhn, Bernd;Wang, Lisha;Kuglstatter, Andreas;Benz, Jorg;Muller, Stephan;Hochstrasser, Remo;Ottaviani, Giorgio;Xin, Jian;Kirchner, Stephan;Mohr, Susanne;Verry, Philippe;Riboulet, William;Shen, Hong C.;Mayweg, Alexander V.;Amrein, Kurt;Tan, Xuefei research published 《 Discovery of 3-Pyridyl Isoindolin-1-one Derivatives as Potent, Selective, and Orally Active Aldosterone Synthase (CYP11B2) Inhibitors》, the research content is summarized as follows. Aldosterone synthase (CYP11B2) inhibitors have been explored in recent years as an alternative therapeutic option to mineralocorticoid receptor (MR) antagonists to reduce elevated aldosterone levels, which are associated with deleterious effects on various organ systems including the heart, vasculature, kidney, and central nervous system (CNS). A benzamide pyridine hit derived from a focused screen was successfully developed into a series of potent and selective 3-pyridyl isoindolin-1-ones CYP11B2 inhibitors. Our systematic structure-activity relationship study enabled us to identify unique structural features that result in high selectivity against the closely homologous cortisol synthase (CYP11B1). We evaluated advanced lead mols., exemplified by compound 52, in an in vivo cynomolgus monkey acute adrenocorticotropic hormone (ACTH) challenge model and demonstrated a superior 100-fold in vivo selectivity against CYP11B1.

141699-55-0, Tert-butyl 3-hydroxyazetidine-1-carboxylate is a useful research compound. Its molecular formula is C8H15NO3 and its molecular weight is 173.21 g/mol. The purity is usually 95%.

Tert-butyl 3-hydroxyazetidine-1-carboxylate has been shown to be a good substrate for the preparation of N-protected amino alcohols and amines by the process of reductive amination. In this synthesis, tert-butyl azetidinium chloride is used as a catalyst in the reaction with sodium hydroxide. The tert-butyl group can be removed using ammonium hydroxide in the presence of a base such as triethylamine. This reaction can be performed on a large scale, making it useful in the manufacture of pharmaceuticals. The efficiency and solubility of this process make it suitable for use as an introduction to other processes involving N-protected amino alcohols or amines., Application In Synthesis of 141699-55-0

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Some low molecular weight alcohols of industrial importance are produced by the addition of water to alkenes. 72824-04-5, formula is C9H17BO2, Ethanol, isopropanol, 2-butanol, and tert-butanol are produced by this general method. Two implementations are employed, the direct and indirect methods. Application In Synthesis of 72824-04-5

Lopez-Grancha, Matilde;Bernardelli, Patrick;Moindrot, Nicolas;Genet, Elisabeth;Vincent, Carine;Roudieres, Valerie;Krick, Alain;Sabuco, Jean-Francois;Machnik, David;Ibghi, Delphine;Pradier, Laurent;Taupin, Veronique research published 《 A novel selective PKR inhibitor restores cognitive deficits and neurodegeneration in Alzheimer disease experimental models》, the research content is summarized as follows. In Alzheimer disease (AD), the double-strand RNA-dependent kinase protein kinase R (PKR )/EIF2AK2 is activated in brain with increased phosphorylation of its substrate eukaryotic initiation factor 2α (eIF2α). AD risk-promoting factors, such as ApoE4 allele or the accumulation of neurotoxic amyloid-β oligomers (AβOs), have been associated with activation of PKR-dependent signaling. Here, we report the discovery of a novel potent and selective PKR inhibitor (SAR439883) and demonstrate its neuroprotective pharmacol. activity in AD exptl. models. In ApoE4 human replacement male mice, 1-wk oral treatment with SAR439883 rescued short-term memory impairment in the spatial object recognition test and dose-dependently reduced learning and memory deficits in the Barnes maze test. Moreover, in AβO-injected male mice, a 2-wk administration of SAR439883 in diet dose-dependently ameliorated the AβO-induced cognitive impairment in both Y-maze and Morris Water Maze, prevented loss of synaptic proteins, and reduced levels of the proinflammatory cytokine interleukin-1β. In both mouse models, these effects were associated with a dose-dependent inhibition of brain PKR activity as measured by both PKR occupancy and partial lowering of peIF2α levels. Our results provide evidence that selective pharmacol. inhibition of PKR by a small selective mol. can rescue memory deficits and prevent neurodegeneration in animal models of AD-like pathol., suggesting that inhibition of PKR is a potential therapeutic approach for AD.

Application In Synthesis of 72824-04-5, Allylboronic acid pinacol ester is a useful research compound. Its molecular formula is C9H17BO2 and its molecular weight is 168.04 g/mol. The purity is usually 95%.
Allylboronic acid pinacol ester is an allylation reagent that is used to produce aldehydes from ketones. It reacts with water, yielding the desired product and formaldehyde as a byproduct. The reaction proceeds through a sequence of steps, in which the boronate ester first reacts with water to form an allylboronate ion and hydrogen gas. This intermediate then reacts with potassium t-butoxide to produce the desired allyl alcohol and potassium borohydride. Finally, the palladium complex catalyst reduces the carbonyl group of the starting material, converting it into an aldehyde. Allylboronic acid pinacol ester is commercially available as a white solid, but can also be synthesized from 2-chloro-5-pinacolylborane (pinacol) in high yield using catalytic cross coupling reactions., 72824-04-5.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts