Category: 4442-53-9

Recommanded Product: 4442-53-9, Having gained chemical understanding at molecular level, chemistry graduates may choose to apply this knowledge in almost unlimited ways, as it can be used to analyze all matter and therefore our entire environment. 4442-53-9, Name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid,introducing its new discovery.

New sildenafil analogues containing an ether ring fused into the phenyl moiety, 6a-d and 7a-d, were efficiently synthesized from the readily available starting materials, 1a-d and 2, in five steps. Ab initio calculations indicated that introduction of a cyclic ether to the phenyl group might enhance the co-planarity of the molecule. The torsional angles were calculated to be 2-3 for the 5-membered cyclic ether derivatives, 6a, 6c, 7a, and 7c, and 12-16 for the 6-membered ones, 6b, 6d, 7b, and 7d. On the other hand, sildenafil showed the least co-planarity with the torsional angle of 23 compared with the target compounds, 6a-d and 7a-d. in the enzyme assay, however, the in vitro PDE 5 inhibitory activity was found out to be inversely related to the degree of co-planarity. In other words, the least planar sildenafil showed the highest actiivty, and the most planar 5-membered cyclic ether derivatives were least active by 100-200-fold compared with sildenafil. Our study clearly demonstrated that the open chain 2′-alkoxy group of the phenyl ring, although less effective for inducing the co-planarity, seemed to act as a much better lipophilic requirement than the cyclic alkoxy moiety. Copyright

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Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Synthetic Route of 4442-53-9,New Advances in Chemical Research in 2021. The appropriate choice of redox mediator can avoid electrode passivation and overpotential, which strongly inhibit the efficient activation of substrates in electrolysis. 4442-53-9, Name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid,introducing its new discovery.

The process development and improvements for route selection, adapted to large scale for the pilot-scale preparation of SL65.0102-10, an N-diazabicyclo[2.2.2]-octylmethyl benzamide, a 5-HT3 and 5-HT4 receptor active ligand for the treatment of neurological disorders such as cognition impairment, are described in this article. Notable steps and enhancements are compared to the original route, including the improvement of a chiral epoxide synthesis by shortening the number of chemical steps, the deprotection of a quaternary ammonium salt, and the redesign of the final amidification coupling to avoid chromatography.

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Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Research speed reading in 2021.The dynamic chemical diversity of the numerous elements, ions and molecules that constitute the basis of life provides wide challenges and opportunities for research. COA of Formula: C9H8O4, In a article, mentioned the application of 4442-53-9, Name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, molecular formula is C9H8O4

While acid fluorides can readily be made from widely available or biomass-feedstock-derived carboxylic acids, their use as functional groups in metal-catalyzed cross-coupling reactions is rare. This report presents the first demonstration of Pd-catalyzed decarbonylative functionalization of acid fluorides to yield trifluoromethyl arenes (ArCF3). The strategy relies on a Pd/Xantphos catalytic system and the supply of fluoride for transmetalation through intramolecular redistribution to the the Pd center. This strategy eliminated the need for exogenous and detrimental fluoride additives and allows Xantphos to be used in catalytic trifluoromethylations for the first time. Our experimental and computational mechanistic data support a sequence in which transmetalation by R3SiCF3 occurs prior to decarbonylation.

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Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Electric Literature of 4442-53-9, Research speed reading in 2021. The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic. In a document type is Patent, and a compound is mentioned, 4442-53-9, Name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, introducing its new discovery.

Compounds of the general formula (I): STR1 where A, R1, R2, R3, R4, R5 and R6 are defined in the description. Medicinal products.

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Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

New discoveries in chemical research and development in 2021. We’ll be discussing some of the latest developments in chemical about CAS: 4442-53-9,name: 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, In a article, mentioned the application of 4442-53-9, molecular formula is C9H8O4

A novel and efficient approach for direct carbonation of aromatic acids with ethyl bromodifluoroacetate as the carbonyl source is reported. A broad range of substrates bearing various functional groups were tolerated, leading to monoalkyl phthalate derivatives in moderate to good yields.

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Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

New research progress on 4442-53-9 in 2021. In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. Recommanded Product: 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, In a article, mentioned the application of 4442-53-9, Name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, molecular formula is C9H8O4

AK3 compounds are mitotic arrest agents that induce high levels of gH2AX during mitosis and apoptosis following release from arrest. We synthesized a potent AK3 derivative, AK306, that induced arrest and apoptosis of the HCT116 colon cancer cell line with an EC50 of approximately 50 nmol/L. AK306 was active on a broad spectrum of cancer cell lines with total growth inhibition values ranging from approximately 25 nmol/L to 25 mmol/L. Using biotin and BODIPY-linked derivatives of AK306, binding to clathrin heavy chain (CLTC/CHC) was observed, a protein with roles in endocytosis and mitosis. AK306 inhibited mitosis and endocytosis, while disrupting CHC cellular localization. Cells arrested in mitosis by AK306 showed the formation of multiple microtubule-organizing centers consisting of pericentrin, g-tubulin, and Aurora A foci, without apparent centrosome amplification. Cells released from AK306 arrest were unable to form bipolar spindles, unlike nocodazole-released cells that reformed spindles and completed division. Like AK306, CHC siRNA knockdown disrupted spindle formation and activated p53. A short-term (3-day) treatment of tumor-bearing APC-mutant mice with AK306 increased apoptosis in tumors, but not normal mucosa. These findings indicate that targeting the mitotic CHC complex can selectively induce apoptosis and may have therapeutic value. Implication: Disruption of clathrin with a small-molecule inhibitor, AK306, selectively induces apoptosis in cancer cells by disrupting bipolar spindle formation.

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Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Application of 4442-53-9, Research speed reading in 2021. The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic. In a document type is Patent, and a compound is mentioned, 4442-53-9, Name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, introducing its new discovery.

Substituted piperazine compounds of formula I STR1 in which HET is a substituted pyrazole, imidazole or 1,2,4-triazole have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson’s disease, obesity, hypertension, Tourette’s syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer’s disease, senile dementia, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.

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Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Chemical Research Letters, May 2021. The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. Which mentioned a new discovery about Recommanded Product: 4442-53-9, Recommanded Product: 4442-53-9

New sildenafil analogues containing an ether ring fused into the phenyl moiety, 6a-d and 7a-d, were efficiently synthesized from the readily available starting materials, 1a-d and 2, in five steps. Ab initio calculations indicated that introduction of a cyclic ether to the phenyl group might enhance the co-planarity of the molecule. The torsional angles were calculated to be 2-3 for the 5-membered cyclic ether derivatives, 6a, 6c, 7a, and 7c, and 12-16 for the 6-membered ones, 6b, 6d, 7b, and 7d. On the other hand, sildenafil showed the least co-planarity with the torsional angle of 23 compared with the target compounds, 6a-d and 7a-d. in the enzyme assay, however, the in vitro PDE 5 inhibitory activity was found out to be inversely related to the degree of co-planarity. In other words, the least planar sildenafil showed the highest actiivty, and the most planar 5-membered cyclic ether derivatives were least active by 100-200-fold compared with sildenafil. Our study clearly demonstrated that the open chain 2′-alkoxy group of the phenyl ring, although less effective for inducing the co-planarity, seemed to act as a much better lipophilic requirement than the cyclic alkoxy moiety. Copyright

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Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Synthetic Route of 4442-53-9, Chemical Research Letters, May 2021. The appropriate choice of redox mediator can avoid electrode passivation and overpotential, which strongly inhibit the efficient activation of substrates in electrolysis. 4442-53-9, Name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid,introducing its new discovery.

The discovery and SAR of potent, selective dioxane-fused tricyclic benz[d]imidazole derivatives as mPGES-1 inhibitor are herein described. Various amide modifications in this series afforded many potent mPGES-1 inhibitors, of which 17d proved to be suitable for further profiling in vivo. Compound 17d {2-((2-chloro-6-fluorophenyl)amino)-N-(3-fluoro-5-(trifluoromethyl)phenyl)-1-methyl-7,8-dihydro-1H-[1,4]dioxino[2?,3?:3,4]benzo[1,2-d]imidazole-5-carboxamide} exhibited excellent mPGES-1 enzyme (IC50: 8 nM), cell (A549 IC50: 16.24 nM) and human whole blood potency (IC50: 249.9 nM). In rodent species, 17d strongly inhibited guinea pig mPGES-1 (IC50: 10.79 nM), but not the rat and mouse enzyme. Furthermore 17d displayed excellent in vitro selectivity over mPGES-2, cPGES, COX-enzymes (COX-1, 2), selectivity against other prostanoid synthases, favorable hERG and CEREP panel profile. Likewise, our lead 17d demonstrated good oral pharmacokinetic profiles and good CNS B/P ratio in rat and guinea pig. Lead 17d also unveiled good efficacy in LPS-induced thermal hyperalgesia pain model with ED50of 36.7 mg/kg, respectively.

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Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Research speed reading in 2021. The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic. name: 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, In a article, mentioned the application of 4442-53-9, Name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, molecular formula is C9H8O4

Pharmaceutical compositions of the invention comprise functionalized benzamide derivatives useful as pregenomic RNA encapsidation inhibitors, and are useful for the treatment of Hepatitis B virus (HBV) infection.

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Reference：
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem