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A simple synthesis of nitriles from aldoximes

Easily synthesized aldoximes have been converted to the corresponding nitriles under very mild conditions by a simple reaction with lH-benzotriazol-l-yloxytris(dimethylamino)phosphonium hexafluorophosphate (BOP) and DBU in CH2CI2, THF, or DMF. As an alternative reagent that eliminates the formation of hexamethylphosphoramide as a byproduct, use of lH-benzotriazol-lyl-4-methylbenzenesulfonate (Bt-OTs) and DBU was investigated. Reactions with this reagent also proceeded smoothly and in good yields, although in one case N-sulfonylation was observed. An attempt to gain mechanistic insight into the BOP-mediated reaction has been made using 31P{ 1H} NMR. However, no phosphorus-bearing intermediate could be readily observed. Finally, the method has been applied to the synthesis of an antiviral 4′-cyano adenosine analogue from a commercial precursor using a single saccharide protecting group.

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Benzofuran – Wikipedia,
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Carboxylic Esters as Radical Leaving Groups: A New and Efficient Gas-phase Synthesis of Benzofurans

Flash vacuum pyrolysis (FVP) of o-allyloxycinnamate esters gives benzofurans in high yield, via cyclisation of a phenoxyl radical and subsequent cleavage of the carboxylic ester function; coumarins are obtained by FVP of the corresponding phenols.

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Chloro-oxime derivatives as novel small molecule chaperone amplifiers

Chloro-oxime derivatives were investigated as novel small molecule chaperone amplifiers. Lead optimization led to the discovery of compounds that displayed potent HSF1 activation activity, significant cytoprotection in MG-132 stress, ER stress and PolyQ stress cell models (EC50 < 10 muM). One of the oldest and most widely used commercial enzyme inhibitors is aspirin, Formula: C9H5NO, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 41717-32-2

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Evidence for Phthalimidonitrene as a Common Intermediate in Several Extrusion Reactions

A common intermediate, presumably phthalimidonitrene 1, is generated in the thermolysis of the aziridinobenzofurans 3 (R = Ac, CO2Me, Bz, COBut and CN) as well as the sulphimide 4, and the azabenzonorbornadiene 5.The transfer of 1 shown in Scheme 1 is zero order in 2-acetylbenzofuran providing further evidence against a concerted bimolecular mechanism 10 for ‘nitrene’ transfer.

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A Mild TEMPO-Catalyzed Aerobic Oxidative Conversion of Aldehydes into Nitriles

An efficient method to prepare nitriles from aldehydes using hexamethyldisilazane (HMDS) as the nitrogen source has been developed. The reactions were performed with 2,2,6,6-tetramethylpiperidine l-oxyl (TEMPO) as the catalyst, NaNO2 or TBN as the co-catalyst, and molecular oxygen as the terminal oxidant under mild conditions. A variety of aromatic, heteroaromatic, aliphatic and allylic aldehydes could be converted into their corresponding nitriles in good to excellent yields.

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Reactivity of Benzo[b]furans: A full perspective

Benzofuran derivatives and benzofuransare presented as scaffolds in complex molecules and have attracted much attention and prevalent interest due to their interesting biological activity. They also exist in several numbers of naturally occurring compounds and exhibiting biological activity. In this review, we will try to underscore the reactivity of benzofurans through comprehension and giving a full perspective to the readers.

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New one-step synthesis of 2-aryl-1H-imidazoles: Dehydrogenation of 2-aryl-delta2-imidazolines with dimethylsulfoxide

A new one-step method for the preparation of 2-aryl-1Himidazoles 3, based on the DMSO dehydrogenation of 2-aryl-Delta2-imidazolines, is described. A comparative study between DMSO and 10% Pd/C, the best known catalyst employed in this transformation, has also been developed. Both protocols were carried out at 120 C for 48 hours.

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A Transition-Metal-Free One-Pot Cascade Process for Transformation of Primary Alcohols (RCH2OH) to Nitriles (RCN) Mediated by SO2F2

A new transition-metal-free one-pot cascade process for the direct conversion of alcohols to nitriles was developed without introducing an ?additional carbon atom?. This protocol allows transformations of readily available, inexpensive, and abundant alcohols to highly valuable nitriles.

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Insect toxins from an endophytic fungus from wintergreen

Two new compounds, 5-hydroxy-2-(1′-oxo-5′-methyl-4′-hexenyl)benzofuran (1) and 5-hydroxy-2-(1′-hydroxy-5′-methyl-4′-hexenyl)benzofuran (2), have been isolated via bioassay-directed fractionation of culture extracts of an unidentified endophytic fungus obtained from wintergreen, Gaultheria procumbens L. Their structures have been deduced from spectral data and confirmed by synthesis. Both 1 and 2 show toxicity to spruce budworm (Christoneura fumiferana Clem.) cells, and 1 is also toxic to the larvae.

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Anthranilic acid derivatives as inhibitors of the cGMP-phosphodiesterase

Compounds of formula (I) STR1where R 1 is hydrogen; R 2 is nitro, cyano or halo(lower)alkyl; R 3 is phenyl substituted with one or more substituents selected from halogen, cyano and lower alkoxy; A is a lower alkylene group; R 4 is a group CR 6 R 7 R 8 wherein R 6 and R 7 form, together with the carbon atom to which they are attached a cycloalkyl group optionally substituted with hydroxy, lower alkoxy or a lower alkanoylamino; and R 8 is hydrogen; its prodrug and a salt thereof.

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