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A series of fluorinated protoberberines have been prepared by condensing fluorinated phthalide anions with 6,7-dimethoxydihydroisoquinoline. The spectroscopy and stereochemistry of the products are discussed and the stereochemical outcome of the reactions rationalised.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1537O – PubChem

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A series of n-butylphthalide derivatives were designed and synthesized. The in vitro activities of these compounds were evaluated by a resting tension of isolated rat thoracic aorta ring assay. Compounds 4g and 4i were found to be more active than n-butylphthalide.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1536O – PubChem

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Pd(II)-catalyzed C-H lactonization of o-methyl benzoic acid substrates has been achieved using molecular oxygen as the oxidant. This finding provides a rare example of C-H oxygenation through Pd(II)/Pd(0) catalysis as well as a method to construct biologically important benzolactone scaffolds. The use of a gas mixture of 5% oxygen in nitrogen demonstrated the possibility for its application in pharmaceutical manufacturing.

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Benzofuran – Wikipedia,
Benzofuran | C8H1534O – PubChem

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CS-758 was selected as a candidate for clinical trials, but since its water-solubility was insufficient for an injectable formulation, phosphoryl ester prodrugs were designed. In this study, the synthesis and evaluation of these injectable prodrugs are described. Phosphoryl ester 17h was soluble in water, and was stable in both water and in a solid state. 17h was converted to CS-758 in human liver microsome and was also converted to CS-758 in rats after intravenous (i.v.) administration with good conversion speed and efficiency. 17h (i.v.) reduced the viable cell counts in kidneys in a murine hematogenous Candida albicans infection model and in lungs in a murine pulmonary Aspergillus fumigatus infection model, wherein the effects were comparable to or slightly superior to that of CS-758 (per os).

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1531O – PubChem

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Selective alpha-oxidation of ethers under aerobic conditions is a long-pursued transformation; however, a green and efficient catalytic version of this reaction remains challenging. Herein, we report a new family of iron catalysts capable of promoting chemoselective alpha-oxidation of a range of ethers with excellent mass balance and high turnover numbers under 1 atm of O2 with no need for any additives. Unlike metalloenzymes and related biomimetics, the catalyst produces H2 as the only byproduct. Mechanistic investigations provide evidence for an unexpected two-step reaction pathway, which involves dehydrogenative incorporation of O2 into the ether to give a peroxobisether intermediate followed by cleavage of the peroxy bond to form two ester molecules, releasing stoichiometric H2 gas in each step. The operational simplicity and environmental friendliness of this methodology affords a useful alternative for performing oxidation, while the unique ability of the catalyst in oxygenating a substrate via dehydrogenation points to a new direction for understanding metalloenzymes and designing new biomimetic catalysts.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1527O – PubChem

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The present invention is substituted with phthalazinone derivatives, the phthalazinone derivative of pharmaceutical compositions comprising the same are disclosed. In particular it relates to poly (ADP – ribose) polymerase inhibit the activity of pharmaceutical compositions of for phthalazinone derivatives are disclosed. (by machine translation)

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Benzofuran – Wikipedia,
Benzofuran | C8H1522O – PubChem

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Two difluorinated analogues of FPL 64176 (methyl 4-(2-benzylbenzoyl)-2,5-dimethylpyrrole-3-carboxylate) have been synthesized in three steps from 6-fluorophthalide and methyl 2,5-dimethylpyrrole-3-carboxylate. Significant overlap of signals was observed in the aromatic regions of the 1H NMR spectra of these compounds. Using 1H-{1H} and 1H-{19F} NOE difference spectroscopy it was possible to identify and assign all aromatic resonances and, based on the NOEs observed, differentiate between the positional isomers and definitely assign the structure of each.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1530O – PubChem

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3-Nitroindenoisoquinoline human topoisomerase IB (Top1) poisons have potent antiproliferative effects on cancer cells. The undesirable nitro toxicophore could hypothetically be replaced by other functional groups that would retain the desired biological activities and minimize potential safety risks. Eleven series of indenoisoquinolines bearing 3-nitro bioisosteres were synthesized. The molecules were evaluated in the Top1-mediated DNA cleavage assay and in the National Cancer Institute’s 60 cell line cytotoxicity assay. The data reveal that fluorine and chlorine may substitute for the 3-nitro group with minimal loss of Top1 poisoning activity. The new information gained from these efforts can be used to design novel indenoisoquinolines with improved safety.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1525O – PubChem

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A series of 11-[4-(cinnamyl)-1-piperazinyl]-6,11-dihydrodibenz[b,e]oxepins and related compounds were synthesized and evaluated for their protective activities against complete ischemia, normobaric hypoxia, lipidperoxidation and convulsion. Structure-activity relationship studies of this series led to the finding of (E)-1-(3-fluoro-6,11-dihydrodibenz[b,e]oxepin-11-yl)-4-(3-phenyl-2-prop enyl)piperazine dimaleate (50), AJ-3941 with the most appropriate property for combined pharmacological activities. Compound 50 also shows an inhibitory effect against cerebral edema as well when orally given to rats.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1532O – PubChem

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A new catalytic system that employs water as an environmentally friendly solvent for the dehydrogenative oxidation of alcohols and lactonization of diols has been developed. In this catalytic system, a water-soluble dicationic iridium complex having a functional ligand that comprises alpha-hydroxypyridine and 4,5-dihydro-1H-imidazol-2-yl moieties exhibits high catalytic performance. For example, the catalytic dehydrogenative oxidation of 1-phenylethanol in the presence of 0.25 mol % of the iridium catalyst and base under reflux in water proceeded to give acetophenone in 92% yield. Additionally, under similar reaction conditions, the iridium-catalyzed dehydrogenative lactonization of 1,2-benzenedimethanol gave phthalide in 98% yield.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1539O – PubChem