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Direct decarboxylative radical allylation of aliphatic carboxylic acids is described. With K2S2O8 as the oxidant and AgNO3 as the catalyst, the reactions of aliphatic carboxylic acids with allyl sulfones in aqueous CH3CN solution gave the corresponding alkenes in satisfactory yields under mild conditions. This site-specific allylation method is applicable to all primary, secondary, and tertiary alkyl acids and exhibits wide functional group compatibility.

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

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Disclosed are derivatives of protoberberine biological alkaloids or physiologically acceptable salts thereof produced by means of a derivative reaction of a source material of biological alkaline quaternary ammonium salts of protoberberine alkaloids, a preparation method for same and pharmaceutical uses thereof. The derivatives of protoberberine biological alkaloids or the physiologically acceptable salts thereof show activity inhibiting ulcerative colitis and can be used in the preparation of drugs for same.

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

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A novel and efficient silver catalyzed decarboxylative direct C2-alkylation of benzothiazoles with carboxylic acids for the synthesis of 2-alkyl benzothiazoles was developed.

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

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The design, synthesis, and structure-activity relationship of 3-oxybenzamides as potent inhibitors of the coagulation protease factor Xa are described on the basis of X-ray structures, privileged structure motifs, and SAR information. A total of six X-ray structures of fXa/inhibitor complexes led us to identify the major protein-ligand interactions. The binding mode is characterized by a lipophilic dichlorophenyl substituent interacting with Tyr228 in the protease S1 pocket, while polar parts are accommodated in S4. This alignment in combination with docking allowed derivation of 3D-QSAR models and tailored scoring functions to rationalize biological affinity and provide guidelines for optimization. The resulting models showed good correlation coefficients and predictions of external test sets. Furthermore, they correspond to binding site topologies in terms of steric, electrostatic, and hydrophobic complementarity. Two approaches to derive tailored scoring functions combining binding site and ligand information led to predictive models with acceptable predictions of the external set. Good correlations to experimental affinities were obtained for both AFMoC (adaptation of fields for molecular comparison) and the novel TScore function. The SAR information from 3D-QSAR and tailored scoring functions agrees with all experimental data and provides guidelines and reasonable activity estimations for novel fXa inhibitors.

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

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An I2-promoted one-pot protocol was proposed for the synthesis of 2-aryl-3-(pyridine-2-ylamino)imidazo[1,2-a]pyridines from aromatic ketones and 2-aminopyridines. The present reaction proceeded well in the presence of I2 in DMSO, and it avoided the requirement of any metal, base, and ligand.

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

Discover the magic of the C10H10O3

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The Pd-catalyzed direct C(sp2)-H arylation of aromatic ketones using a transient directing group is described. The ketimine/carboxylate bidentate directing group in situ generated from aromatic ketone and glycine enabled a palladium-catalyzed ortho-C-H arylation, which shows extensive substrate compatibility.

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

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The synthesis of some cyclic and open analogues of 2-(2,6-dimethoxyphenoxyethylaminomethyl)-1,4-benzodioxane (1, WB 4101) is described. The blocking activity of this compound and its analogues (1-5) was determined on the pre- and postsynaptic alpha-adrenoceptors of isolated rat vas deferens to investigate the structural requirements for conpetitive alpha-adrenoceptor occupancy by antagonists of the benzodioxane class. The activities of 1-5 at the presynaptic alpha-adrenoceptor were not significantly different whereas there were differences among the compounds of at least two orders of magnitude at the postsynaptic alpha-adrenoceptor. This clearly indicates that the structural requirements at the presynaptic receptor level are less restrictive than those required by the postsynaptic alpha-adrenoceptor. The symmetric analogues 3 and 4 were significantly weaker postsynaptic alpha-antagonists compared to 1. On the other hand, 2 and 5 displayed a very high postsynaptic activity, almost comparable to that of 1. These findings might suggest that the antagonists of the benzodioxane class do not bind at two identical aromatic sites symmetrically arranged around the anionic site of the alpha-adrenoceptor. Indeed, they might indicate that the benzodioxane binding site(s) incorporates two areas with very similar but not identical structural requirements. Furthermore, the very high activity of 5 may suggest that the benzodioxane nucleus is not essential to activity.

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

Archives for Chemistry Experiments of 1-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)ethanone

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It has been shown by 1H NMR spectroscopy that hydrazones obtained by the condensation of hydrazides of [5-4-pyridyl)-1,3,4-oxadiazol-2-ylthio]acetic or 2-[5-(2-pyridyl)-1,3,4-oxadiazol-2-ylthio]propionic acids with aldehydes, ketones, and beta-dicarbonyl compounds exist in DMSO solution as a mixture of stereoisomeric forms.

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

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A series of pyrazoles derived from the substituted enaminones were synthesized and were evaluated for antimicrobial activity. All the compounds were characterized by the spectral data and elemental analysis. The synthesized compounds were initially screened for their antimicrobial activity against ATCC 6538, NCTC 10400, NCTC 10418, and ATCC 27853. During initial screening, compounds (P1, P6, and P11) presented significant antimicrobial activity through disc diffusion assay. These compounds were further evaluated for antimicrobial activity at different time points against Gram-positive and Gram-negative bacteria and presented significant activity for 6 hours. The activity was found to be greater against Gram-positive bacteria. In contrast at 24 hours, the activity was found only against Gram-positive bacteria except compound (P11), showing activity against both types of bacteria. Compound (P11) was found to have highest activity against both Gram-positive and Gram-negative bacteria.

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

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Disclosed is a compound of Formula (I). Also disclosed is a method of treating spinal muscular atrophy, as well as methods of using such compounds to increase SMN expression, increase EAAT2 expression, or increase the expression of a nucleic acid that encodes a translational stop codon introduced directly or indirectly by mutation or frameshift

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