Category: 22483-09-6

Wang, Xianheng published the artcilePreparation of Dolutegravir Intermediate Diastereomer, Safety of 2,2-Dimethoxyethanamine, the main research area is dolutegravir tricyclic intermediate diastereoselective preparation.

A convenient method was developed to prepare the diastereomer of dolutegravir tricyclic intermediate in the catalysis of EDCI/DMAP in up to 87% yield. Different solvents, temperature, and times were optimized. The synthesized diastereomer 6′ could be used as a standard for the industrial manufacture requirement of dolutegravir active pharmaceutical ingredient.

Journal of Heterocyclic Chemistry published new progress about Cyclization. 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

Hussain, Mulla Althafh published the artcileTotal synthesis of (±)-aspidostomide B, C, regioisomeric N-methyl aspidostomide D and their derivatives, HPLC of Formula: 22483-09-6, the main research area is aspidostomide B C D analog regioselective synthesis; cyclization total synthesis aspidostomide B C D; dehydration total synthesis aspidostomide B C D; regioselective ring opening total synthesis aspidostomide B C D.

A full account of the total synthesis of aspidostomide B, C, their analogs and our synthetic efforts towards the synthesis of aspidostomide D, which led to the synthesis of regioisomeric N-Me aspidostomide D, its analogs via epoxide opening strategy is presented. The synthesis of regioisomeric N-Me aspidostomide D involves an efficient, five-step sequence, with 36.3% overall yield, starting from 3,4,5-tribromo-1H-pyrrole-2-carboxylic acid. The key features of this protocol are intramol. cyclization, dehydration, oxidation, and a Lewis acid-mediated regioselective epoxide ring opening by C-3 position of 2,5-dibromo-1H-indole to furnish the title compounds

Tetrahedron Letters published new progress about Cyclization. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, HPLC of Formula: 22483-09-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Xi, Hancheng published the artcileSterically hindered diarylethenes with thienopyridine: Substituent position effect on photochromic properties, Computed Properties of 22483-09-6, the main research area is photochromism sterically hindered diarylethenes thienopyridine NMR; substituent effect photochromism sterically hindered diarylethenes thienopyridine.

Diarylethenes (DAEs) have recently attracted great attention for their applications in light-responsive materials. As much efforts have been directed towards the elucidation of the structure-property relationship of DAE derivatives, improving photochromic performances through structure optimization is still worthy of study. Herein, three isomeric diarylethenes with thienopyridine units are designed for gaining insights into substituent position effect on photochromic performances. It is shown that the nitrogen atom in pyridine rings shows influence on the photochromic behaviors, such as photoreaction quantum yields, conversion ratios of target systems. Distinctively, thieno [3,2-b]pyridine-containing I (TP3) displays a novel solvent-dependent photochromic activity. And the photochromic reactivity of thieno [2,3-b]pyridine-containing II (TP1) can be specifically blocked by Cu2+, showing the gated photochromism. The diverse photochromic properties make the target systems promising candidates for the development of practical mol. devices with certain functions.

Dyes and Pigments published new progress about Conformation. 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

Yang, Tao published the artcileStudy the lipidoid nanoparticle mediated genome editing protein delivery using 3D intestinal tissue model, Safety of 2,2-Dimethoxyethanamine, the main research area is lipidoid nanoparticle genome editing protein delivery intestinal tissue model; 3D tissue model; Genome engineering; Lipidoid nanoparticle; Oral drug delivery; Protein delivery.

Lipid nanoparticles are promising carriers for oral drug delivery. For bioactive cargos with intracellular targets, e.g. gene-editing proteins, it is essential for the cargo and carrier to remain complexed after crossing the epithelial layer of intestine in order for the delivery system to transport the cargos inside targeted cells. However, limited studies have been conducted to verify the integrity of cargo/carrier nanocomplexes and their capability in facilitating cargo delivery intracellularly after the nanocomplex crossing the epithelial barrier. Herein, we used a traditional 2D transwell system and a recently developed 3D tissue engineered intestine model and demonstrated the synthetic lipid nanoparticle (carrier) and protein (cargo) nanocomplexes are able to cross the epithelial layer and deliver the protein cargo inside the underneath cells. We found that the EC16-63 LNP efficiently encapsulated the GFP-Cre recombinase, penetrated the intestinal monolayer cells in both the 2D cell culture and 3D tissue models through temporarily interrupting the tight junctions between epithelial layer. After transporting across the intestinal epithelia, the EC16-63 and GFP-Cre recombinase nanocomplexes can enter the underneath cells to induce gene recombination. These results suggest that the in vitro 3D intestinal tissue model is useful for identifying effective lipid nanoparticles for potential oral drug delivery.

Bioactive Materials published new progress about Cell culture. 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

Meng, Ning published the artcileDesign and semisynthesis of oleanolic acid derivatives as VEGF inhibitors: Inhibition of VEGF-induced proliferation, angiogenesis, and VEGFR2 activation in HUVECs, Product Details of C4H11NO2, the main research area is semisynthesis oleanolic acid derivative VEGF inhibitor VEGFR2 angiogenesis; Angiogenesis; Oleanolic acid; Structural modification; VEGF inhibitor; VEGFR2.

Angiogenesis inhibitors targeting the VEGF signaling pathway are developed into drugs for the treatment of vaious diseases, such as cancer, rheumatoid arthritis, and age-related macular degeneration. Recent studies have revealed that oleanolic acid (OA), a natural pentacyclic triterpenoid, inhibited the VEGF/VEGFR2 signaling pathway and angiogenesis in HUVECs, which may represent an attractive VEGF inhibitor. In this paper, rational structural modification towards OA was performed in order to improve its inhibitory effects aganist VEGF and anti-angiogenesis potential. As a result, a series of novel OA derivatives, possessing α,β-unsaturated ketone system in ring A and amide functional group at C-28, were prepared and evaluated for cytotoxicity and their ability to inhibit VEGF-induced abnormal proliferation of HUVECs. The results showed that two promising derivatives, OA-1 and OA-16, exhibited no in vitro cytotoxicity against HUVECs but showed more potent inhibitory activity against VEGF-induced proliferation and angiogenesis in HUVECs, compared with OA. The results of Western blot indicated that OA-1 and OA-16 inhibited VEGF-induced VEGFR2 activation. Furthermore, small interfering RNA experiments were performed to confirm that both compounds inhibited VEGF-induced angiogenesis via VEGFR2. Thus, the present study resulted in the discovery of new promising OA-inspired VEGF inhibitors, which can serve as potential lead compounds for the treatment of angiogenesis-related diseases.

Chinese Journal of Natural Medicines (Amsterdam, Netherlands) published new progress about Angiogenesis. 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

Li, Yanqing published the artcileBis(N-acylated imidazolin-2-imine) nickel catalyzed norbornene copolymerization with methyl acrylate, Product Details of C4H11NO2, the main research area is imidazolin imine catalyzed norbornene methyl acrylate copolymerization.

The incorporation of even a small number of polar functional groups in the polyolefin backbone is sufficient to improve the polyolefin properties. Compared with palladium catalyzed direct copolymerization of olefins with polar vinyl monomers, the development of low-cost nickel-based catalysts is more challenging because of their higher oxophilicity. On the basis of the advantage of reducing the electrophilicity of the nickel center by the installation of strongly electron-donating ligands, we herein report the synthesis of novel bis(N-acylated imidazolin-2-imine) nickel complexes for norbornene polymerization and copolymerization with polar monomers. Moreover, the Ph substituent on the imidazoline ligand is expected to enhance the tolerance of the nickel catalyst toward polar functional groups, thus allowing the copolymerization of norbornene with com. Me acrylate to afford high mol. weight functionalized cyclic olefin copolymers (COCs) with moderate activity and reasonable comonomer content.

Polymer Chemistry published new progress about Contact angle. 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

Amador-Sanchez, Yoarhy A. published the artcileDiversity-Oriented Synthesis of Highly Fluorescent Fused Isoquinolines for Specific Subcellular Localization, Category: alcohols-buliding-blocks, the main research area is fluorescent fused isoquinoline cell.

A multicomponent diversity-oriented synthesis of new highly emissive tetracyclic isoquinolines that target specific organelles is described. The title compounds were prepared via a three-step protocol starting with an Ugi four-component reaction, followed by either an intramol. alkyne hydroarylation and subsequent alkene isomerization or through a Pomeranz-Fritsch-type cyclization with a final intramol. Heck reaction. Subcellular localization studies of these compounds using green channel confocal microscopy revealed remarkable and distinctive distribution patterns in live cells, showing an unprecedented high selectivity and imaging contrast. The differentiated organelle visualization-including localizers for mitochondria, lysosomes, Golgi apparatus, endoplasmic reticulum, and plasma membrane-was achieved by varying the nature of the tetracyclic system and substituent pattern, changing the original four-component set in the starting Ugi reaction.

Journal of Organic Chemistry published new progress about Cell membrane. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, Category: alcohols-buliding-blocks.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Han, Jinhe published the artcileMolecular design, synthesis, and biological evaluation of bisamide derivatives as cyclophilin A inhibitors for HCV treatment, Recommanded Product: 2,2-Dimethoxyethanamine, the main research area is bisamide preparation mol design docking SAR antiviral human; Bisamide; Cyclophilin A inhibitor; Hepatitis C virus; Molecular modeling; Ugi reaction.

Hepatitis C virus (HCV) is a major cause of end-stage liver diseases. Direct-acting antivirals including inhibitors of nonstructural proteins (NS3/4A protease, NS5A, and NS5B polymerase), represent key components of anti-HCV treatment. Previous reports have shown that bisamides could be a novel class of cyclophilin A (CypA) inhibitors for treating HCV as a member of combinational therapies. To fully elucidate SARs of bisamide derivatives and find a better hit compound with diverse binding modes, sixteen bisamides I (R1 = Cy, t-Bu; R2 = C6H5, 3,4-MeO2C6H3, 3,4,5-MeO3C6H2, 2,3,4-MeO3C6H2; R3 = C6H5, 4-MeOC6H4, 4-BrC6H4, etc.; R4 = indol-2-yl, 1-(4-methoxybenzyl)-1H-indol-3-ylmethyl, 1H-indol-3-ylmethyl) were designed with the help of docking program. They were then synthesized using one-pot four-component Ugi reaction. Compound I (R1 = Cy; R2 = 3,4,5-MeO3C6H2; R3 = (3,4-dimethoxyphenyl)ethyl; R4 = 1H-indol-3-ylmethyl) with selectivity index of more than 18.9 (50% effective concentration of 5.3μM, but no cytotoxicity at 100μM) and unique binding mode that could be dived into gatekeeper pocket was selected as a new hit compound Surface plasmon resonance experiments revealed that the above compound is able to bind to CypA with a KD of 3.66μM. Taken together, these results suggest that the above compound as a CypA inhibitor could be used as an alternative anti-HCV agent in combinational therapy in the future.

European Journal of Medicinal Chemistry published new progress about Antiviral agents. 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

Sun, Chiyu published the artcileSynthesis and Evaluation of Aminothiazole Derivatives as Hedgehog Pathway Inhibitors, HPLC of Formula: 22483-09-6, the main research area is aminothiazole Hedgehog inhibitor antitumor neoplasm; Gli1, hedgehog signaling; Smo; aminothiazole; benzimidazole; cytotoxicity; synthesis.

A series of aminothiazole derivatives bearing the benzimidazole moiety were synthesized and evaluated in Gli luciferase reporter assays. Lead optimization led to the discovery of potent hedgehog pathway antagonist (I) (2-[3-(1H-benzimidazol-2-yl)-4-chloroanilino]-N-[4-(trifluoromethyl)phenyl]-1,3-thiazole-4-carboxamide), with IC50 values in nanomolar range. The mol. basis ascribed to hindering sonic hedgehog-driven Smoothened (Smo) localization within the primary cilium (PC). Moreover, compound I inhibited Gli1 mRNA expression in mutant Smo cell line and displayed moderate cytotoxicity against DAOY cancer cell.

Chemistry & Biodiversity published new progress about Antitumor agents. 22483-09-6 belongs to class alcohols-buliding-blocks, name is 2,2-Dimethoxyethanamine, and the molecular formula is C4H11NO2, HPLC of Formula: 22483-09-6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Lin, Hong published the artcileDiscovery of Potent and Selective Covalent Protein Arginine Methyltransferase 5 (PRMT5) Inhibitors, Quality Control of 22483-09-6, the main research area is covalent inhibitor PRMT5 hemiaminals cocrystal structure.

Protein arginine methyltransferase 5 (PRMT5) is known to sym. dimethylate numerous cytosolic and nuclear proteins that are involved in a variety of cellular processes. Recent findings have revealed its potential as a cancer therapeutic target. PRMT5 possesses a cysteine (C449) in the active site, unique to PRMT5. Therefore, covalent PRMT5 inhibition is an attractive chem. approach. Herein, we report an exciting discovery of a series of novel hemiaminals that under physiol. conditions can be converted to aldehydes and react with C449 to form covalent adducts, which presumably undergo an unprecedented elimination to form the thiol-vinyl ethers, as indicated by electron d. in the co-crystal structure of the PRMT5/MEP50 complex.

ACS Medicinal Chemistry Letters published new progress about Antitumor agents. 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