The important role of 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid

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CONDENSED RING DERIVATIVE, AND PREPARATION METHOD, INTERMEDIATE, PHARMACEUTICAL COMPOSITION AND USE THEREOF

Disclosed are a condensed ring derivative, and a preparation method, an intermediate, a pharmaceutical composition and a use thereof. The condensed ring derivative of the present invention has a significant inhibitive effect on URAT1, which can effectively alleviate or treat hyperuricemia and other related diseases.

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

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Palladium-Catalyzed Carboxylate-Assisted Ethoxycarboxylation of Aromatic Acids to Synthesize Monoethyl Phthalate Derivatives with Ethyl Bromodifluoroacetate

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

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Pilot scale process development of SL65.0102-10, an N-diazabicyclo[2.2.2]-octylmethyl Benzamide

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

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Substituted 2,3-alkylene bis (oxy) benzamides and derivatives and method of preparation

Novel substituted 2,3-alkylene bis (oxy) benzamides and derivatives thereof are disclosed. Also disclosed is a method for producing said compounds. The compounds have anxiolytic, psychostimulant, disinhibiting and thymoanaleptic properties useful therapeutically in the psychofunctional field, particularly in gastro-enterology, cardiology, urology, rheumatology and gynaecology.

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

Archives for Chemistry Experiments of 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid

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SWEET FLAVOR MODIFIER

The present invention includes compounds having structural formula (I), or pharmaceutically acceptable salts, solvate, and/or ester thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of ingestible compositions. Furthermore, the present invention provides methods for preparing the compounds.

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

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Palladium-Catalyzed Decarbonylative Trifluoromethylation of Acid Fluorides

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

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Containing 1, 4 – benzodioxane of benzene and 1, 2, 4 – triazole class derivative and its preparation and its antibacterial activity (by machine translation)

A containing 1, 4 – benzodioxane of benzene and 1, 2, 4 – triazole class derivatives, has the following general formula: In the formula R is: The invention containing 1, 4 – benzodioxane of benzene and 1, 2, 4 – triazole class derivatives to the bacillus subtilis (B. subtilis), Staphylococcus aureus (S. aureus), Escherichia coli (E.coli), Pseudomonas aeruginosa (P. aeruginosa) is markedly inhibited, so this invention containing 1, 4 – benzodioxane of 1, 2, 4 – triazole class derivatives can be in preparing antibacterial drug application. The invention discloses the preparation method. (by machine translation)

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

Extracurricular laboratory:new discovery of 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid

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Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766)

Demonstrating intracellular protein target engagement is an essential step in the development and progression of new chemical probes and potential small molecule therapeutics. However, this can be particularly challenging for poorly studied and noncatalytic proteins, as robust proximal biomarkers are rarely known. To confirm that our recently discovered chemical probe 1 (CCT251236) binds the putative transcription factor regulator pirin in living cells, we developed a heterobifunctional protein degradation probe. Focusing on linker design and physicochemical properties, we generated a highly active probe 16 (CCT367766) in only three iterations, validating our efficient strategy for degradation probe design against nonvalidated protein targets.

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

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AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS

Specific Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein m, X, R1, R2, R3, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the com?pounds and using the compounds for treatment of dis?eases associated with LRRK2 receptor, such as Parkin?son?s disease

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

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Rhodium(I)-catalyzed regiospecific dimerization of aromatic acids: Two direct C-H bond activations in water

2,2′-Diaryl acids are key building blocks for some of the most important and high-performance polymers such as polyesters and polyamides (imides), as well as structural motifs of MOFs (metal-organic frameworks) and biological compounds. In this study, a direct, regiospecific and practical dimerization of simple aromatic acids to generate 2,2′-diaryl acids has been discovered, which proceeds through two rhodium-catalyzed C-H activations in water. This reaction can be easily scaled up to gram level by using only 0.4-0.6 mol% of the rhodium catalyst. As a proof-of-concept, the natural product ellagic acid was synthesized in two steps by this method. On the double: An efficient, regiospecific, and general oxidative dimerization of simple aryl acids to generate diaryl acids was developed. The reaction involves two direct aryl C-H activations catalyzed by rhodium, uses water as the solvent, and can be easily scaled up. The natural product ellagic acid was obtained in only two steps by using this method.

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