Category: 22483-09-6

Hoang, Van-Hai published the artcileDiscovery of Conformationally Restricted Human Glutaminyl Cyclase Inhibitors as Potent Anti-Alzheimer’s Agents by Structure-Based Design, Formula: C4H11NO2, the main research area is Alzheimer’s disease glutaminyl cyclase SAR conformational analysis.

Alzheimer’s disease (AD) is an incurable, progressive neurodegenerative disease whose pathogenesis cannot be defined by one single element but consists of various factors; thus, there is a call for alternative approaches to tackle the multifaceted aspects of AD. Among the potential alternative targets, we aim to focus on glutaminyl cyclase (QC), which reduces the toxic pyroform of β-amyloid in the brains of AD patients. On the basis of a putative active conformation of the prototype inhibitor 1, a series of N-substituted thiourea, urea, and α-substituted amide derivatives were developed. The structure-activity relationship analyses indicated that conformationally restrained inhibitors demonstrated much improved QC inhibition in vitro compared to nonrestricted analogs, and several selected compounds demonstrated desirable therapeutic activity in an AD mouse model. The conformational anal. of a representative inhibitor indicated that the inhibitor appeared to maintain the Z-E conformation at the active site, as it is critical for its potent activity.

Journal of Medicinal Chemistry published new progress about Alzheimer disease. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Formula: C4H11NO2.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Cheng, Zhi-Qiang published the artcileMolecular-docking-guided design and synthesis of new IAA-tacrine hybrids as multifunctional AChE/BChE inhibitors, Product Details of C4H11NO2, the main research area is indoleacetic acid tacrine synthesis antiAlzheimer pharmacokinetics acetylcholinesterase butyrylcholinesterase; Alzheimer’s disease; Dual AChE/BChE inhibitor; IAA-tacrine hybrids; Molecular docking; Neural network electrical activity.

A series of new indole-3-acetic acid (IAA)-tacrine hybrids as dual acetylcholinesterase (AChE)/butyrylcholinesterase (BChE) inhibitors were designed and prepared based on the mol. docking mode of AChE with an IAA derivative (1a), a moderate AChE inhibitor identified by screening our compound library for anti-Alzheimer’s disease (AD) drug leads. The enzyme assay results revealed that some hybrids, e.g. 5d and 5e, displayed potent dual in vitro inhibitory activities against AChE/BChE with IC50 values in low nanomolar range. Mol. modeling studies in tandem with kinetic anal. suggest that these hybrids target both catalytic active site and peripheral anionic site of cholinesterase (ChE). Mol. dynamic simulations and Mol. Mechanics/Poisson-Boltzmann Surface Area (MM-PBSA) calculations indicate that 5e has more potent binding affinity than hit 1a, which may explain the stronger inhibitory effect of 5e on AChE. Furthermore, their predicted pharmacokinetic properties and in vitro influences on mouse brain neural network elec. activity were discussed. Taken together, compound 5e can be highlighted as a lead compound worthy of further optimization for designing new anti-AD drugs.

Bioorganic Chemistry published new progress about Alzheimer disease. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Product Details of C4H11NO2.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Gorecki, Lukas published the artcilePhenothiazine-Tacrine Heterodimers: Pursuing Multitarget Directed Approach in Alzheimer’s Disease, COA of Formula: C4H11NO2, the main research area is phenothiazine tacrine heterodimer preparation Alzheimer’s cholinesterase inhibitor; Alzheimer’s disease; acetylcholinesterase; butyrylcholinesterase; multitarget directed ligands; phenothiazine; tacrine.

Since 2002, no clin. candidate against Alzheimer’s disease has reached the market; hence, an effective therapy is urgently needed. We followed the so-called “”multitarget directed ligand”” approach and designed 36 novel tacrine-phenothiazine heterodimers which were in vitro evaluated for their anticholinesterase properties. The assessment of the structure-activity relationships of such derivatives highlighted compound 1dC as a potent and selective acetylcholinesterase inhibitor with IC50 = 8 nM and 1aA as a potent butyrylcholinesterase inhibitor with IC50 = 15 nM. Selected hybrids, namely, 1aC, 1bC, 1cC, 1dC, and 2dC, showed a significant inhibitory activity toward τ(306-336) peptide aggregation with percent inhibition ranging from 50.5 to 62.1%. Likewise, 1dC and 2dC exerted a remarkable ability to inhibit self-induced Aβ1-42 aggregation. Notwithstanding, in vitro studies displayed cytotoxicity toward HepG2 cells and cerebellar granule neurons; no pathophysiol. abnormality was observed when 1dC was administered to mice at 14 mg/kg (i.p.). 1dC was also able to permeate to the CNS as shown by in vitro and in vivo models. The maximum brain concentration was close to the IC50 value for acetylcholinesterase inhibition with a relatively slow elimination half-time. 1dC showed an acceptable safety and good pharmacokinetic properties and a multifunctional biol. profile.

ACS Chemical Neuroscience published new progress about Alzheimer disease. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, COA of Formula: C4H11NO2.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Reeves, Benjamin M. published the artcileTransition-Metal-Free Reductive Hydroxymethylation of Isoquinolines, Safety of 2,2-Dimethoxyethanamine, the main research area is isoquinolinium iodide paraformaldehyde reductive hydroxymethylation Cannizzaro Evans Tishchenko; hydroxymethylated tetrahydroisoquinoline preparation; potassium methoxide isoquinolinium iodide paraformaldehyde methylation hydroxymethylation tandem; tetrahydroisoquinoline one pot preparation; formaldehyde; reductive-functionalization; tandem reaction; tetrahydroisoquinoline; transition-metal-free synthesis.

A transition-metal-free reductive hydroxymethylation reaction has been developed, enabling the preparation of tetrahydroisoquinolines, e.g., I, bearing C4-quaternary centers from the corresponding isoquinolines. Deuterium labeling studies and control experiments enable a potential mechanism to be elucidated which features a key Cannizzaro-type reduction followed by an Evans-Tishchenko reaction. When isoquinolines featuring a proton at the 4-position are used, a tandem methylation-hydroxymethylation occurs, leading to the formation of II with 2 new C-C bonds in one pot.

Angewandte Chemie, International Edition published new progress about C-C bond formation. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Safety of 2,2-Dimethoxyethanamine.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Reedy, E. D. Jr. published the artcileInterfacial toughness: dependence on surface roughness and test temperature, COA of Formula: C4H11NO2, the main research area is aluminum epoxy interface surface roughness temperature.

Abstract: Interfacial toughness quantifies resistance to crack growth along an interface and in this investigation the toughness of an aluminum/epoxy interface was measured as a function of surface roughness and test temperature The large strain response of the relatively ductile epoxy adhesive used in this study was also characterized. This epoxy adhesive exhibits intrinsic strain-softening after initial compressive yield and then deforms plastically at a roughly constant flow stress until it rapidly hardens at large compressive strains. We find that interface toughness scales as the product of the temperature dependent epoxy yield strength and a length scale that characterizes surface roughness. The proposed scaling is based upon dimensional considerations of a model problem that assumes that the characteristic length scale of both the roughness and the crack-tip yield zone is small relative to the region dominated by the linear elastic asymptotic crack-tip stress field. Furthermore, the model assumes that interfacial failure occurs only after the epoxy begins to harden at large strains. The proposed relationship is validated by our interfacial toughness measurements.

International Journal of Fracture published new progress about Interface roughness. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, COA of Formula: C4H11NO2.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Derasp, Joshua S. published the artcileRhodium-Catalyzed Synthesis of Amides from Functionalized Blocked Isocyanates, Quality Control of 22483-09-6, the main research area is rhodium catalyst coupling boroxine blocked masked isocyanate; synthesis amide.

Isocyanates are useful building blocks for the synthesis of amides, although their widespread use has been limited by their high reactivity, which often results in poor functional group tolerance and a propensity to oligomerize. Herein, a rhodium-catalyzed synthesis of amides is described coupling boroxines with blocked (masked) isocyanates. The success of the reaction hinges on the ability to form both the isocyanate and the organorhodium intermediates in situ. Relying on masked isocyanate precursors and on the high reactivity of the organorhodium intermediate results in broad functional group tolerance, including protic nucleophilic groups such as amines, anilines, and alcs.

ACS Catalysis published new progress about Amides Role: SPN (Synthetic Preparation), PREP (Preparation). 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Quality Control of 22483-09-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Khodadadi, Meysam published the artcileOne-pot synthesis of novel spirocyclic-dihydropyrazine-2-(1H)ones through a Ugi 4-CR/deprotection, Recommanded Product: 2,2-Dimethoxyethanamine, the main research area is cycloalkanone benzoic acid isocyanocyclohexane dimethoxyethanamine tandem Ugi cyclization deprotection; benzoyl cyclohexyl spirodihydropyrazinone preparation.

A one-pot approach for the synthesis of new spirocyclic-dihydropyrazine-2-(1H)ones was described. The Ugi four-component condensation of cycloalkanones, carboxylic acids, cyclohexyl isocyanide and aminoacetaldehyde di-Me acetal followed by acid-catalyzed deprotection-cyclization afforded the desired products in moderate to good yields.

Journal of Heterocyclic Chemistry published new progress about Benzoic acids Role: RCT (Reactant), RACT (Reactant or Reagent). 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Recommanded Product: 2,2-Dimethoxyethanamine.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Singh, Sangh Priya published the artcileSynthesis of β- and γ-lactam fused dihydropyrazinones from Ugi adducts via a sequential ring construction strategy, Computed Properties of 22483-09-6, the main research area is amino oxophenylethyl dimethoxyethyl phenylpropiolamide regioselective cycloisomerization; diphenyl pyrrolopyrazinedione preparation; benzylidene phenyl diazabicyclooctenedione preparation.

A modular approach for the construction of β- and γ-lactam fused dihydropyrazinones from the readily available Ugi adducts was described. The sequential construction of rings through base-mediated cycloisomerization followed by acid-mediated cyclization yielded β-lactam fused dihydropyrazinones. However, the Ugi-derived dihydropyrazinones afforded γ-lactam fused dihydropyrazinones under base-mediated cycloisomerization. The regioselectivity in the cycloisomerization reactions was explained on the basis of ring-strain. Substrate scope, limitations and mechanistic investigations through DFT-calculations was explored.

Chemical Communications (Cambridge, United Kingdom) published new progress about Benzaldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Computed Properties of 22483-09-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Srinivasachary, K. published the artcilePractical and Efficient Route to Dolutegravir Sodium via One-Pot Synthesis of Key Intermediate with Controlled Formation of Impurities, COA of Formula: C4H11NO2, the main research area is dolutegravir sodium preparation green chem.

An efficient, cost effective and com. viable synthesis of dolutegravir sodium has been developed from com. available I as the key intermediate. The key features of the synthesis are lower number of synthetic steps and the use of eco-friendly and inexpensive reagents. The process has been demonstrated to meet ICH requirements on scaling up.

Russian Journal of Organic Chemistry published new progress about Aralkyl amines Role: RCT (Reactant), RACT (Reactant or Reagent). 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, COA of Formula: C4H11NO2.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Ghandi, Mehdi published the artcileA combined multicomponent-acid catalyzed cyclization reaction as an efficient route to novel tricyclic pyrrolo[2,1-a]isoquinoline derivatives, SDS of cas: 22483-09-6, the main research area is tricyclic pyrroloisoquinoline preparation; polysubstituted pyrrole preparation heterocyclization sulfuric acid catalyst; arylglyoxal cyclic dicarbonyl dimethoxyethanamine keto ester four component Knoevenagel.

A simple, new two-step procedure for the synthesis of novel tricyclic pyrrolo[2,1-a]isoquinoline derivatives I (R = H, Me, Cl, Ph; R1 = 2-hydroxy-4,4-dimethyl-6-oxocyclohex-1-en-1-yl, 2-hydroxy-6-oxocyclohex-1-en-1-yl, 4-hydroxy-2-oxo-2H-chromen-3-yl; R2 = Me, Et) is described. The initially prepared polysubstituted pyrroles II via the four-component condensation of arylglyoxals 4-RC6H4C(O)CHO, cyclic 1,3-dicarbonyls such as 1,3-cyclohexanedione, 5,5-dimethyl-1,3-cyclohexanedione, 4-hydroxy-2H-chromen-2-one, aminoacetaldehyde di-Me acetal and β-keto esters R2OC(O)CH2C(O)CH3 subsequently underwent intramol. acid-catalyzed cyclization to give the desired products in moderate to good yields I.

Journal of Heterocyclic Chemistry published new progress about Cyclic diketones Role: RCT (Reactant), RACT (Reactant or Reagent). 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, SDS of cas: 22483-09-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts