Category: 4739-94-0

New discoveries in chemical research and development in 2021. Reactions catalyzed within inorganic and organic materials and at electrochemical interfaces commonly occur at high coverage. In a patent，Which mentioned a new discovery about name: Ethyl 2,3-dihydrobenzo[1,4]dioxine-2-carboxylate, name: Ethyl 2,3-dihydrobenzo[1,4]dioxine-2-carboxylate

The present disclosure relates to compounds of Formula (I): (I); and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as autoinflammatory and autoimmune diseases and cancers.

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

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The affinity of ligands for either the 5-HT2A or 5-HT2C agonist binding site was enhanced by modification of the 2,5-oxygen substituents that are found in typical hallucinogenic amphetamines such as 4b (DOB). Restriction of the conformationally flexible 2,5-dimethoxy substituents into fused dihydrofuran rings generally resulted in increased potency relative to the parent 2,5-dimethoxy compounds. The pure enantiomers of these arylalkylamines were obtained by enantiospecific synthesis that involved acylation of the heterocyclic nucleus 7 with N-trifluoroacetyl-protected D- or L-alanyl chloride, followed by ketone reduction and N-deprotection. The enantiomers demonstrated modest stereoselectivity at the two receptors. Several general trends within these classes of new compounds were observed during their pharmacological investigation. For most pairs of optical isomers tested, the R-enantiomers of the compounds containing heterocycle 7 bound with only slightly higher affinity than their S-antipodes at the 5-HT2A and 5-HT2C receptors. Likewise, functional studies indicated that the R-enantiomers generally displayed increased potency compared to the S-enantiomers. Aromatization of the dihydrofuran rings of these arylalkylamines further increased affinity and potency. Only a few compounds were full agonists with most of them possessing intrinsic activities in the range of 60-80%. These compounds with a fully aromatic linear tricyclic nucleus are some of the highest-affinity ligands for the 5-HT2A receptor reported to date.

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

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. HPLC of Formula: C11H12O4, However, they have proven to be challenging because of the mutual inactivation of both catalysts. 4739-94-0, name is Ethyl 2,3-dihydrobenzo[1,4]dioxine-2-carboxylate. In an article，Which mentioned a new discovery about 4739-94-0

Dihydrobenzofuran analogues of hallucinogens. 3. Models of 4-substituted (2,5-dimethoxyphenyl)alkylamine derivatives with rigidified methoxy groups

Tetrahydrobenzodifuran functionalities were employed as conformationally restricted bioisosteres of the aromatic methoxy groups in prototypical hallucinogenic phenylalkylamines 1 and 2. Thus, a series of 8-substituted 1- (2,3,6,7-tetrahydrobenzo[1,2-b:4,5-b’]difuran-4-yl)-2-aminoalkanes (7a-e) were prepared and evaluated for activity in the two-lever drug discrimination paradigm in rats trained to discriminate saline from LSD tartrate (0.08 mg/kg) and for the ability to displace [3H]ketanserin from rat cortical homogenate 5-HT(2A) receptors and [3H]-8-OH-DPAT from rat hippocampal homogenate 5-HT(1A) receptors. In addition, 1-(8-bromo-2,3,6,7- tetrahydrobenzo[1,2-b:4,5-b’]difuran-4-yl)-2-aminopropane (7b), which was found to be extremely potent in the rat in vivo assays, was evaluated for its ability to compete with [125I]DOI and [3H]ketanserin binding to cells expressing cloned human 5-HT(2A), 5-HT(2B), and 5-HT(2C) receptors. All of the dihydrofuranyl compounds having a hydrophobic substituent para to the alkylamine side chain had activities in both the in vitro and in vivo assays that equaled or surpassed the activity of the analogous conformationally flexible parent compounds. For example, 7b substituted for LSD in the drug discrimination assay with an ED50 of 61 nmol/kg and had K(i) values in the nanomolar to subnanomolar range for the displacement of radioligand from rat and human 5-HT2 receptors, making it one of the most potent hallucinogen- like phenylalkylamine derivatives reported to date. The results suggest that the dihydrofuran rings in these new analogues effectively model the active binding conformations of the methoxy groups of the parent compounds 1 and 2. In addition, the results provide information about the topography and relative orientation of residues involved in agonist binding in the serotonin 5-HT2 receptors.

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

In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. COA of Formula: C11H12O4, 4739-94-0, name is Ethyl 2,3-dihydrobenzo[1,4]dioxine-2-carboxylate. In an article，Which mentioned a new discovery about 4739-94-0

Novel benzodifuran analogs as potent 5-HT2A receptor agonists with ocular hypotensive activity

A series of 8-substituted benzodifuran analogs was prepared and evaluated for 5-HT2A receptor binding and activation. Several compounds containing ether and ester functionality were found to be potent agonists. Topical ocular administration of 5, 18, and 25 effectively reduced intra-ocular pressure in the hypertensive cynomolgus monkey eye in the range of 25-37%.

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

Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner.In a patent, 4739-94-0, name is Ethyl 2,3-dihydrobenzo[1,4]dioxine-2-carboxylate, introducing its new discovery. Recommanded Product: 4739-94-0

Synthesis of Dihydrobenzofurans from Phenolic Mannich Bases and their Quaternized Derivatives

Reaction of dimethylsulphoxonium methylide with quaternized derivatives of phenolic Mannich bases, and in certain cases with the bases themselves, constitutes a useful synthesis of dihydrobenzofurans.On the other hand treatment of those same quaternized derivatives with diazomethane may be a useful alternative procedure for the preparation of coumarans with base-sensitive groups.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

In classical electrochemical theory, both the electron transfer rate and the adsorption of reactants at the electrode control the electrochemical reaction. SDS of cas: 4739-94-0, 4739-94-0, name is Ethyl 2,3-dihydrobenzo[1,4]dioxine-2-carboxylate. In an article£¬Which mentioned a new discovery about 4739-94-0

Synthesis and cytotoxic activity of novel tetrahydrobenzodifuran?imidazolium salt derivatives

The synthesis of a series of novel 4-substituted 2,3,6,7-tetrahydrobenzo [1,2-b;4,5-b?]difuran?1H-imidazolium salts is presented. The biological properties of the compounds were evaluated in vitro against a panel of human tumor cell lines. Results suggest that the 5,6-dimethyl-benzimidazole or 2-methyl-benzimidazole ring, and substitution of the imidazolyl-3-position with a 2-naphthylmethyl substituent or 2-naphthylacyl substituent, were important to the cytotoxic activity. Notably, 3-(2-Naphthylmethyl)-1-((2,3,6,7-tetrahydrobenzo[1,2-b;4,5-b?]difuran-4-yl)methyl)-1H-5,6-dimethyl-benzimidazol-3-ium bromide (42) was found to be the most potent derivative against five human tumor cell lines with IC50 values of 1.06?4.34?muM and more selective towards SMMC-7721, A549 and SW480 cell lines. 3-(2-Naphthylacyl)-1-((2,3,6,7-tetrahydrobenzo[1,2-b;4,5-b?]difuran-4-yl)methyl)-1H-2-methyl-benzimidazol-3-ium bromide (37) showed higher selectivity to SMMC-7721 and MCF-7 cell lines with IC50 values 2.7-fold and 8.4-fold lower than DDP. Study regarding to the antitumor mechanism of action showed that compound 37 could induce cell cycle G1 phase arrest and apoptosis in SMMC-7721 cells.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. Safety of Ethyl 2,3-dihydrobenzo[1,4]dioxine-2-carboxylate. Introducing a new discovery about 4739-94-0, Name is Ethyl 2,3-dihydrobenzo[1,4]dioxine-2-carboxylate

SELECTIVE INHIBITORS OF NLRP3 INFLAMMASOME

The present disclosure relates to compounds of Formula (I): (I); and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as autoinflammatory and autoimmune diseases and cancers.

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Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Electric Literature of 4739-94-0, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, and a compound is mentioned, 4739-94-0, Ethyl 2,3-dihydrobenzo[1,4]dioxine-2-carboxylate, introducing its new discovery.

Enantiospecific synthesis and pharmacological evaluation of a series of super-potent, conformationally restricted 5-HT2A/2C receptor agonists

The affinity of ligands for either the 5-HT2A or 5-HT2C agonist binding site was enhanced by modification of the 2,5-oxygen substituents that are found in typical hallucinogenic amphetamines such as 4b (DOB). Restriction of the conformationally flexible 2,5-dimethoxy substituents into fused dihydrofuran rings generally resulted in increased potency relative to the parent 2,5-dimethoxy compounds. The pure enantiomers of these arylalkylamines were obtained by enantiospecific synthesis that involved acylation of the heterocyclic nucleus 7 with N-trifluoroacetyl-protected D- or L-alanyl chloride, followed by ketone reduction and N-deprotection. The enantiomers demonstrated modest stereoselectivity at the two receptors. Several general trends within these classes of new compounds were observed during their pharmacological investigation. For most pairs of optical isomers tested, the R-enantiomers of the compounds containing heterocycle 7 bound with only slightly higher affinity than their S-antipodes at the 5-HT2A and 5-HT2C receptors. Likewise, functional studies indicated that the R-enantiomers generally displayed increased potency compared to the S-enantiomers. Aromatization of the dihydrofuran rings of these arylalkylamines further increased affinity and potency. Only a few compounds were full agonists with most of them possessing intrinsic activities in the range of 60-80%. These compounds with a fully aromatic linear tricyclic nucleus are some of the highest-affinity ligands for the 5-HT2A receptor reported to date.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Electric Literature of 4739-94-0. In my other articles, you can also check out more blogs about 4739-94-0

Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Application In Synthesis of Ethyl 2,3-dihydrobenzo[1,4]dioxine-2-carboxylate, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 4739-94-0, Name is Ethyl 2,3-dihydrobenzo[1,4]dioxine-2-carboxylate, molecular formula is C11H12O4

Synthesis and cytotoxic activity of novel tetrahydrobenzodifuran?imidazolium salt derivatives

The synthesis of a series of novel 4-substituted 2,3,6,7-tetrahydrobenzo [1,2-b;4,5-b?]difuran?1H-imidazolium salts is presented. The biological properties of the compounds were evaluated in vitro against a panel of human tumor cell lines. Results suggest that the 5,6-dimethyl-benzimidazole or 2-methyl-benzimidazole ring, and substitution of the imidazolyl-3-position with a 2-naphthylmethyl substituent or 2-naphthylacyl substituent, were important to the cytotoxic activity. Notably, 3-(2-Naphthylmethyl)-1-((2,3,6,7-tetrahydrobenzo[1,2-b;4,5-b?]difuran-4-yl)methyl)-1H-5,6-dimethyl-benzimidazol-3-ium bromide (42) was found to be the most potent derivative against five human tumor cell lines with IC50 values of 1.06?4.34?muM and more selective towards SMMC-7721, A549 and SW480 cell lines. 3-(2-Naphthylacyl)-1-((2,3,6,7-tetrahydrobenzo[1,2-b;4,5-b?]difuran-4-yl)methyl)-1H-2-methyl-benzimidazol-3-ium bromide (37) showed higher selectivity to SMMC-7721 and MCF-7 cell lines with IC50 values 2.7-fold and 8.4-fold lower than DDP. Study regarding to the antitumor mechanism of action showed that compound 37 could induce cell cycle G1 phase arrest and apoptosis in SMMC-7721 cells.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Application In Synthesis of Ethyl 2,3-dihydrobenzo[1,4]dioxine-2-carboxylate, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 4739-94-0, in my other articles.

Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. category: benzodioxans. Introducing a new discovery about 4739-94-0, Name is Ethyl 2,3-dihydrobenzo[1,4]dioxine-2-carboxylate

Synthesis of Dihydrobenzofurans from Phenolic Mannich Bases and their Quaternized Derivatives

Reaction of dimethylsulphoxonium methylide with quaternized derivatives of phenolic Mannich bases, and in certain cases with the bases themselves, constitutes a useful synthesis of dihydrobenzofurans.On the other hand treatment of those same quaternized derivatives with diazomethane may be a useful alternative procedure for the preparation of coumarans with base-sensitive groups.

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.category: benzodioxans, you can also check out more blogs about4739-94-0

Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem