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Preparing a cosmetic additive 2 – (benzofuran -2 – yl) benzoxazole new method (by machine translation)

The invention relates to a technical field of fine chemicals, discloses a process for preparing cosmetic additive 2 – (benzofuran – 2 – yl) benzoxazole new method. Specific steps: to benzoxazole with benzofuran – 2 – carboxylic acid as the raw material, nickel chloride as catalyst, silver carbonate and 1, 3 – double (2, 6 – diisopropyl phenyl) imidazole chloride as an additive, in chlorobenzene 160 degree Celcius reaction 20 hours, to obtain 2 – (benzofuran – 2 – yl) benzoxazole. Compared with the prior art, this method has simple and rapid, one-step direct constructing target product. In addition, the use of inexpensive, easy to store of the carboxylic acid as the coupling reagent, with potential industrial value, is worthy of application. (by machine translation)

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Synthesis of condensed heteroaromatic compounds by palladium-catalyzed oxidative coupling of heteroarene carboxylic acids with alkynes

The palladium-catalyzed oxidative coupling of indole-3-carboxylic acids with alkynes effectively proceeds in a 1:2 manner accompanied by decarboxylation to produce the corresponding 1,2,3,4-tetrasubstituted carbazoles, some of which exhibit solid-state fluorescence. Pyrrole-, benzofuran-, and furancarboxylic acids also undergo the decarboxylative coupling to afford highly substituted indole, dibenzofuran, and benzofuran derivatives, respectively.

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Benzofuran – Wikipedia,
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Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs)

We report the synthesis and evaluation of a series of heterobiaryl amides as positive allosteric modulators of mGluR4. Compounds 9b and 9c showed submicromolar potency at both human and rat mGluR4. In addition, both 9b and 9c were shown to be centrally penetrant in rats using nontoxic vehicles, a major advance for the mGluR4 field.

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Benzofuran – Wikipedia,
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Reaction of aryl-2-hydroxypropenoic derivatives with boron tribromide

(Z)-Mono, di or trimethoxyphenyl-2-hydroxypropenoic acids 1a-d gave mixtures of (E) and (Z) mono, di or trihydroxyphenyl-2-hydroxypropenoic acids 2a-d when treated with boron tibromide. The isomerisation proceeds during the work-up and depends on the duration of the hydrolysis and the number of oxygens on the aromatic ring. When the aromatic ring was substituted with a methoxy group at the ortho position, a cyclisation occurs, and 3-hydroxycoumarins 3 and benzofuran-2-carboxylic acids 4 can be obtained. 3-Hydroxycoumarin 3a can also be obtained almost quatitatively from the reaction of methyl 3-(2-methoxyphenyl)-2,3-epoxypropanoate with boron tribromide.

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Benzofuran – Wikipedia,
Benzofuran | C8H1787O – PubChem

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Lead optimization of a pyridine-carboxamide series as DGAT-1 inhibitors

The structure-activity relationship studies of a novel series of carboxylic acid derivatives of pyridine-carboxamides as DGAT-1 inhibitors is described. The optimization of the initial lead compound 6 based on in vitro and in vivo activity led to the discovery of key compounds 10j and 17h.

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Benzofuran – Wikipedia,
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Preparation of functional styrenes from biosourced carboxylic acids by copper catalyzed decarboxylation in PEG

A general protocol for the copper-catalyzed decarboxylation of alpha,beta-unsaturated carboxylic acids in PEG, particularly of biosourced cinnamic acid analogues, is reported. Moderate to high isolated yields (31-96%) towards the styrene derivatives were obtained. For the first time, decarboxylation of alpha-amino acids to the corresponding amines was successfully performed with good to high yields and extended to the decarboxylation of a few condensed heterocyclic compounds. Both the use of PEG as a green solvent and direct separation of the pure product of the reaction by distillation permitted the reuse of the solvent and the Cu-based catalytic system over several cycles without deactivation. This was extended to the synthesis of 4-vinylguaiacol on the laboratory scale in an average 92% yield. This journal is the Partner Organisations 2014.

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Benzofuran – Wikipedia,
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Putative kappa opioid heteromers as targets for developing analgesics free of adverse effects

It is now generally recognized that upon activation by an agonist, beta-arrestin associates with G protein-coupled receptors and acts as a scaffold in creating a diverse signaling network that could lead to adverse effects. As an approach to reducing side effects associated with kappa opioid agonists, a series of beta-naltrexamides 3-10 was synthesized in an effort to selectively target putative kappa opioid heteromers without recruiting beta-arrestin upon activation. The most potent derivative 3 (INTA) strongly activated KOR-DOR and KOR-MOR heteromers in HEK293 cells. In vivo studies revealed 3 to produce potent antinociception, which, when taken together with antagonism data, was consistent with the activation of both heteromers. 3 was devoid of tolerance, dependence, and showed no aversive effect in the conditioned place preference assay. As immunofluorescence studies indicated no recruitment of beta-arrestin2 to membranes in coexpressed KOR-DOR cells, this study suggests that targeting of specific putative heteromers has the potential to identify leads for analgesics devoid of adverse effects.

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DIAMINE DERIVATIVE, PROCESS FOR PRODUCING THE SAME AND FUNGICIDE CONTAINING THE DERIVATIVE AS ACTIVE INGREDIENT

It is an object of the invention to provide a novel fungicide which exhibits a wide controlling spectrum against pathogens of various crops, and solves the toleration problem. The diamine derivative represented by the formula (1) and a process for preparation of the same, fungicides comprising the same as an active ingredient are disclosed: [wherein R1 is substituents such as an alkyl group having 1 to 6 carbon atoms and the like, R2 and R5 are each independently substituents such as hydrogen atom, an alkyl group having 1 to 6 carbon atoms and the like, R3 and R4 are each independently substituents such as hydrogen atom, an alkyl group having 1 to 6 carbon atoms and the like, or R3 and R4 may be bonded to each other to form a hydrocarbon ring having 3 to 6 carbon atoms, R6, R7, R8 and R9 are each independently substituents such as hydrogen atom, an alkyl group having 1 to 6 carbon atoms and the like, R10 is a substituent such as hydrogen atom, an alkyl group having 1 to 6 carbon atoms and the like, A is an oxygen atom or a sulfur atom, and Q is an aryl group or a heterocycle].

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Discovery of Novel Allosteric Inhibitors of Deoxyhypusine Synthase

Deoxyhypusine synthase (DHPS) utilizes spermidine and NAD as cofactors to incorporate a hypusine modification into the eukaryotic translation initiation factor 5A (eIF5A). Hypusine is essential for eIF5A activation, which, in turn, plays a key role in regulating protein translation of selected mRNA that are associated with the synthesis of oncoproteins, thereby enhancing tumor cell proliferation. Therefore, inhibition of DHPS is a promising therapeutic option for the treatment of cancer. To discover novel lead compounds that target DHPS, we conducted synthetic studies with a hit obtained via high-throughput screening. Optimization of the ring structures of the amide compound (2) led to bromobenzothiophene (11g) with potent inhibitory activity against DHPS. X-ray crystallographic analysis of 11g complexed with DHPS revealed a dramatic conformational change in DHPS, which suggests the presence of a novel allosteric site. These findings provide the basis for the development of novel therapy distinct from spermidine mimetic inhibitors.

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Benzofuran – Wikipedia,
Benzofuran | C8H1724O – PubChem

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Rhodium(III)-catalyzed C-H activation/annulation with vinyl esters as an acetylene equivalent

The behavior of electron-rich alkenes in rhodium-catalyzed C-H activation/annulation reactions is investigated. Vinyl acetate emerges as a convenient acetylene equivalent, facilitating the synthesis of sixteen 3,4-unsubstituted isoquinolones, as well as select heteroaryl-fused pyridones. The complementary regiochemical preferences of enol ethers versus enol esters/enamides is discussed.

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Benzofuran – Wikipedia,
Benzofuran | C8H2018O – PubChem