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Aminodecarboxylation of unactivated alkanecarboxylic acids has been accomplished utilizing an organic photocatalyst. This operationally simple reaction utilizes readily available carboxylic acids to chemoselectively generate reactive alkyl intermediates that are not accessible via conventional two-electron pathways. The organic radical intermediates are efficiently trapped with electrophilic diazo compounds to provide aminated alkanes.

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

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A novel double decarboxylative cross-coupling catalyzed by copper and silver has been developed. This method provides a practical approach for the flexible synthesis of alkenes and alkynes from the readily affordable substrates.

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

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The identification of a new class of potent and selective ROCK-II inhibitors is presented. Compound 5 (SR-3677) had an IC50 of ?3 nM in enzyme and cell based assays and had an off-target hit rate of 1.4% against 353 kinases, and inhibited only 3 out of 70 nonkinase enzymes and receptors. Pharmacology studies showed that 5 was efficacious in both, increasing ex vivo aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation.

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

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Epidermal Growth Factor Receptor (EGFR) is a transmembrane glycoprotein that constitutes one of the four members of ErbB family of tyrosine kinase receptors. Activation of EGFR leads to autophosphorylation of receptor tyrosine kinase that initiates a cascade of downstream signaling pathways involved in regulating cellular proliferation, differentiation, and survival. EGFR is abnormally activated by various mechanisms like receptor overexpression, mutation, ligand-dependent receptor dimerization, ligand-independent activation and is associated with the development of variety of human cancers. EGFR inhibition is one of the key targets for cancer chemotherapy. Approval of tyrosine kinase inhibitors such as erlotinib, gefitinib, and lapatinib for the treatment of non-small cell lung cancer led to tremendous development of novel EGFR inhibitors in the last decade. Diverse class of chemical compounds from the synthetic origin has been extensively studied. This review highlights the various classes of synthetically derived molecules which have been reported in the last few years as potential EGFR and EGFR/ErbB-2 dual inhibitors. A brief synthetic methodology to access these compounds has been highlighted along with the SAR. We strongly believe that this review will provide a platform to the synthetic chemists and biologists to design and synthesize new and potent compounds that inhibit EGFR and ErbB-2.

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

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Ethyl 1,4-benzodioxan-2-carboxylate is used as an intermediate compound for the production of drug doxazosin mesylate. The title compound was kinetically resolved to get S-enantiomer of ethyl 1,4-benzodioxan 2-carboxylate in a simple lipase catalyzed transesterification reaction. Ethyl acetate was used as reaction medium as well as acyl donor. The influence of the enzyme source and time of reaction on the enantio selectivity of product were studied. Lipase from Candida antartica-B (Novozyme A/S) catalyzed transesterification reaction with good enantio selectivity towards S-enantiomer. The high enantiomeric ratio, E = 160, provided S-2 an acceptable chemical yield (50%) and enantiomeric excess (>95%).

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Fatty acid biosynthesis is essential for bacterial survival. ss-Ketoacyl-acyl carrier protein (ACP) synthase III (FabH), is a particularly attractive antibacterial target, since it is central to the initiation of fatty acid biosynthesis. Three series of 21 cinnamaldehyde acylhydrazone derivatives, A3-9, B3-9, and C3-9, were synthesized and evaluated for FabH-inhibitory activity. Compound B6 showed the most potent biological activity against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Bacillus subtilis (minimum inhibitory concentrations (MICs) values: 1.56-3.13mug/mL) and was comparable with the positive control. Docking simulation by positioning compound B6 in the FabH structure active site was performed to explore the possible binding model.

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

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The thrombin receptor PAR-1 is activated by alpha-thrombin to stimulate cells, including platelets, through the tethered-ligand sequence SFLLRN. We have discovered a novel series of heterocycle-peptide hybrids comprised of a tripeptide segment, such as Cha-Arg-Phe, and an N-terminal heterocyclic group, many of which behave as full PAR-1 agonists. Certain compounds with an aminotriazole group, such as 4 and 16, are nearly as potent as SFLLRN-NH2 in inducing platelet aggregation. Also, some arylethenoyl ‘N-capped’ compounds, such as 52 and 57, exhibit mixed PAR-1 agonist-antagonist activity.

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

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Compounds having the formula STR1 and pharmaceutically acceptable salts thereof wherein R represents 6,7-di(lower alkoxy) or 6,7,8-tri(lower alkoxy); m is 1 or 2, X is –CHR1 — or –CH2 CH2 –; each R1 and R0 may be the same or different and is hydrogen or lower alkyl; each of R2 and R3 is hydrogen, lower alkoxy, lower alkyl, halogen, lower alkanoyl, lower alkoxycarbonyl, –CONR4 R5 or –SO2 NR4 R5 wherein each of R4 and R5 is hydrogen or lower alkyl; processes for their preparation; and their use as regulators of the cardiovascular system, and particularly in the treatment of hypertension.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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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 category: benzodioxans, category: benzodioxans

(R)-1,4-Benzodioxane-2-carboxilic acid (R)-1 was obtained by resolution of the racemic acid 1 with stoichiometric or nonstoichiometric (+)- dehydroabietylamine (+)-2 in high chemical yield and enantiomeric excess. (S)-1 was isolated from the mother liquors of the crystallisation of (R)-1·(+)-2 and its enantiomeric excess maximised by recrystallisation procedures involving a precipitation under kinetic control or, alternatively, by conversion into the methyl ester followed by a single crystallisation. The different mechanisms of the two S enrichments is well explained by the binary phase diagrams of the acid and of the ester, which show that the former is a racemic compound, whereas the latter a conglomerate. The DSC analyses were extended to 2-hydroxymethyl- and 2-mesyloxymethyl-1,4-benzodioxane, establishing that the alcohol forms a racemic compound, while its mesyl ester a conglomerate. On the basis of these results, different resolution strategies can be designed to obtain useful homochiral 2-substituted 1,4-benzodioxanes coupling the resolution of 1 via diastereomeric salt formation with the enantiomeric enrichments by recrystallisations, preferably of its conglomerate forming derivatives.

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

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A straightforward silver-mediated oxidative decarboxylative radical trifluoromethylthiolation reaction of aliphatic carboxylic acid is described. This reaction operates under mild conditions and allows the synthesis of various valuable alkyltrifluoromethylthioethers from abundant alkyl carboxylic acids and convenient nucleophilic AgSCF3 reagent. It provides a practical and efficient approach for the preparation of alkyltrifluoromethylthioethers.

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