Month: July 2021

Application of 70918-54-6, Research speed reading in 2021. The prevalence of solvent effects has motivated developing quantitative kinetic, and theoretical assessments of solvent structures and their interactions with reaction intermediates. In a document type is Article, and a compound is mentioned, 70918-54-6, Name is (S)-1,4-Benzodioxane-2-carboxylic acid, introducing its new discovery.

The synthesis of both enantiomers of 1,4-benzodioxan-2-carboxylic acid 1, a key synthetic intermediate for the therapeutic agents piperoxan, prosympal, dibozane, and doxazosin was achieved with good yields and high enantioselectivities via the Arthrobacter sp. lipase catalyzed kinetic resolution of ester (±)-17a. The influence of the co-solvents and the immobilization of the lipase upon kinetic resolution demonstrated that immobilized whole cells, in the presence of n-butanol as a co-solvent, resulted in the optimal resolution of the substrate (ee ?99%, E = 535) at 258 mmol (50 g/L) substrate concentration.

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

New research progress on 22013-33-8 in 2021. In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. Safety of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, In a article, mentioned the application of 22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, molecular formula is C8H9NO2

The synthesis and evaluation of a series of N,N-bis-heterocyclic-methylamines 1 as isoazaerianin analogues are described. It was demonstrated that the replacement of the 3,4,5-trimethoxyphenyl A-ring present in CA-4, isoCA-4 and isoazaerianin by a quinoline or a quinazoline ring is possible and often beneficiary for a high level of cytotoxicity. We have also showed that a carbazole or an indole nucleus are very effective as B-rings in this series, leading to anti-cancer drugs 1 having a sub-nanomolar level of cytotoxicity (1a: IC50 = 70 pM against HCT116 cells). 1a also display a high level of cytotoxicity against four other human cancer cells and inhibited tubulin assembly at a micromolar level. Moreover, at a concentration of 5 nM, 1a arrested the cellular cycle in G2/M phase of the cellular cycle and induced apoptosis of HCT116 cells. It was also showed that after few hours 1a at a concentration of 10 nM totally disrupted endothelial network formation on Matrigel.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Recommanded Product: 22013-33-8, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 22013-33-8, in my other articles.

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

Electric Literature of 214894-89-0, Chemical Research Letters, May 2021.In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. 214894-89-0, Name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine,introducing its new discovery.

Selective inhibition of neuronal nitric oxide synthase (nNOS) has been shown to prevent brain injury and is important for the treatment of various neurodegenerative disorders. This study shows that not only greater inhibitory potency and isozyme selectivity but more druglike properties can be achieved by fragment hopping. On the basis of the structure of lead molecule 6, fragment hopping effectively extracted the minimal pharmacophoric elements in the active site of nNOS for ligand hydrophobic and steric interactions and generated appropriate lipophilic fragments for lead optimization. More potent and selective inhibitors with better druglike properties were obtained within the design of 20 derivatives (compounds 7-26). Our structure – based inhibitor design for nNOS and SAR analysis reveal the robustness and efficiency of fragment hopping in lead discovery and structural optimization, which implicates a broad application of this approach to many other therapeutic targets for which known druglike small-molecule modulators are still limited.

In the meantime we’ve collected together some recent articles in this area about 214894-89-0 to whet your appetite. Happy reading!

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.

Keep reading other articles of 4442-53-9! Don’t worry, you don’t need a PhD in chemistry to understand the explanations! Synthetic Route of 4442-53-9

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

New research progress on 2879-20-1 in 2021. In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. category: benzodioxans, In a article, mentioned the application of 2879-20-1, Name is 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone, molecular formula is C10H10O3

alpha-Alkyl-, alpha-arylalkyl-, and alpha-aryl-substituted benzyl alcohols were converted into the corresponding symmetrical dibenzyl ethers in the presence of a catalytic amount of 10% aqueous HCl both in methylene chloride and under solvent-free conditions. Analogous reactions in dioxane and on heating afforded mainly the corresponding arylalkenes, whereas symmetrical dibenzyl ethers were formed as minor products.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. name: 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 2879-20-1, in my other articles.

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

Related Products of 214894-89-0, 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. 214894-89-0, Name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine,introducing its new discovery.

Highly selective beta-methylation of alcohols was achieved using an earth-abundant first row transition metal in the air stable molecular manganese complex [Mn(CO)2Br[HN(C2H4PiPr2)2]] 1 ([HN(C2H4PiPr2)2]=MACHO-iPr). The reaction requires only low loadings of 1 (0.5 mol %), methanolate as base and MeOH as methylation reagent as well as solvent. Various alcohols were beta-methylated with very good selectivity (>99 %) and excellent yield (up to 94 %). Biomass derived aliphatic alcohols and diols were also selectively methylated on the beta-position, opening a pathway to ?biohybrid? molecules constructed entirely from non-fossil carbon. Mechanistic studies indicate that the reaction proceeds through a borrowing hydrogen pathway involving metal?ligand cooperation at the Mn-pincer complex. This transformation provides a convenient, economical, and environmentally benign pathway for the selective C?C bond formation with potential applications for the preparation of advanced biofuels, fine chemicals, and biologically active molecules.

Interested yet? This just the tip of the iceberg, You can reading other blog about 214894-89-0

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. Recommanded Product: 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone, In a article, mentioned the application of 2879-20-1, Name is 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone, molecular formula is C10H10O3

1-Diazepin-2-ones have been prepared from 1,4-benzodioxane for the first time.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Product Details of 2879-20-1, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 2879-20-1, in my other articles.

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

New research progress on 3663-79-4 in 2021. In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. name: Methyl 1,4-Benzodioxane-2-carboxylate, In a article, mentioned the application of 3663-79-4, Name is Methyl 1,4-Benzodioxane-2-carboxylate, molecular formula is C10H10O4

Unlike the diastereomeric 1-phenylethylammonium salts, the diastereomeric N-1-phenylethylamides of (S)- and (R)-1,4-benzodioxane-2-carboxylic acid show significant differences in fusibility and solubility so as to be efficiently resolved by precipitation of the less soluble diastereomer (>98% de), while chromatographic purification of the unprecipitated fraction affords the more soluble one (>99% de). Overall, 95% of the former and 80% of the latter are recovered. The hydrolysis of the two resolved amides provides the two acid enantiomers and the resolving amine in quantitative yield and with unchanged stereoisomeric purity.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.name: Methyl 1,4-Benzodioxane-2-carboxylate, you can also check out more blogs about3663-79-4

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 Application In Synthesis of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, Application In Synthesis of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine

Cryptosporidium parasites are important waterborne pathogens of both humans and animals. The Cryptosporidium parvum and Cryptosporidium hominis genomes indicate that the only route to guanine nucleotides is via inosine 5?-monophosphate dehydrogenase (IMPDH). Thus the inhibition of the parasite IMPDH presents a potential strategy for treating Cryptosporidium infections. A selective benzimidazole-based inhibitor of C. parvum IMPDH (CpIMPDH) was previously identified in a high throughput screen. Here we report a structure-activity relationship study of benzimidazole-based compounds that resulted in potent and selective inhibitors of CpIMPDH. Several compounds display potent antiparasitic activity in vitro.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Application In Synthesis of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine, you can also check out more blogs about22013-33-8

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

Research speed reading in 2021.The prevalence of solvent effects has motivated developing quantitative kinetic, spectroscopic, and theoretical assessments of solvent structures and their interactions with reaction intermediates and transition states. Quality Control of 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone, In a article, mentioned the application of 2879-20-1, Name is 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone, molecular formula is C10H10O3

A series of substituted chalcones was synthesised and screened for cytotoxic activity against the K562 human leukaemia cell line. (E)-3-(3′- Hydroxy-4′-methoxyphenyl)-2-methyl-1-(3′,4′,5′-trimethoxyphenyl)-prop-2-en- 1-one [IC50 (K562) 0.21 nM] was found to be the most active. A relationship between the conformation and cytotoxicity of the chalcones is discussed.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Quality Control of 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 2879-20-1, in my other articles.

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