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Methods for the conversion of aliphatic acids to alkyl halides have progressed significantly over the past century, however, the analogous decarboxylative bromination of aromatic acids has remained a longstanding challenge. The development of efficient methods for the synthesis of aryl bromides is of great importance as they are versatile reagents in synthesis and are present in many functional molecules. Herein we report a transition metal-free decarboxylative bromination of aromatic acids. The reaction is applicable to many electron-rich aromatic and heteroaromatic acids which have previously proved poor substrates for Hunsdiecker-type reactions. In addition, our preliminary mechanistic study suggests that radical intermediates are not involved in this reaction, which is in contrast to classical Hunsdiecker-type reactivity. Overall, the process demonstrates a useful method for producing valuable reagents from inexpensive and abundant starting materials.

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A systematic investigation of reductive ring expansion reaction of oximes with diisobutylaluminum hydride (DIBAH) was performed. The reaction regiospecifically provided a variety of unsubstituted bicyclic heterocycles 3a-3g or tricyclic heterocycles 3h, 3j-3l that contained nitrogen attached to an aromatic ring.

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[Problem] to improve carrier mobility of the organic thin-film transistor is a compound, composition, and of an organic semiconductor device. (1) A compound represented by the formula [a]. (X1 – X3 Is, independently, O, S, Te or Se; R1 – R8 At least one alkyl group having at each independently […], […], aryl group or the like, the other, a hydrogen atom or, alkyl, alkenyl, aryl, alkylthio or)[Drawing] no (by machine translation)

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In an effort to identify selective for the estrogen receptor subtype ERbeta, a series of aryl benzthiophenes was synthesized. In a radioligand binding assay and reporter gene assat in HeLa and SH-SY5Y cells, compound were characterized as ERbeta-selective agonists. By targeting ERbeta in the brain, these compounds could lead to drugs able to separate the beneficial effects of estrogens on mood, learning, and memory from side effects such as the stimulation of edometrial and breast cancer.

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Cycloalkylnitrile pyrazole carboxamides as JAK inhibitors useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer are provided

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The present invention discloses compounds according to Formula (I), wherein R1, R3, R4, R5, L1, and Cy are as defined herein. The present invention also provides compounds, methods for the production of said compounds of the invention, pharmaceutical compositions comprising the same and their use in allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 and/or interferons. The present invention also methods for the prevention and/or treatment of the aforementioned diseases by administering a compound of the invention.

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This invention provides novel beta-lactamase inhibitors of the aryl- and heteroarylsulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammonium groups. The compounds inhibit three classes of beta-lactamases and synergize the antibacterial effects of beta-lactam antibiotics (e.g., imipenem and ceftazidime) against those micro-organisms normally resistant to the beta-lactam antibiotics as a result of the presence of the Beta-lactamases. Formula (I) or pharmaceutically acceptable salt thereof.

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Benzothiophene – Wikipedia,
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Anodic fluorination of benzo[b]thiophene derivatives provided a complex mixture of di- and trifluorinated products. On the other hand, anodic fluorination of 3-oxo-2,3-dihydrobenzo[b]thiophene and methyl 3-oxo-2,3-dihydrobenzo[b]thiophene-2-carboxylate gave the corresponding monofluorinated products selectively in moderate yields. Anodic fluorination of methyl alpha-(2-cyanophenylthio)acetate followed by intramolecular cyclization provided 3-amino-2-fluorobenzo[b]thiophene in excellent yield. Georg Thieme Verlag Stuttgart · New York.

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The invention discloses a method for synthesizing aromatic amine compound, characterized in that in accordance with the following two kinds of methods in any method for carrying out: method a: will have the general formula (I) of the alkyl aromatic compound having the general formula (II) with the nitrogen containing compound mixed, oxidizing agent and organic solvent in the presence of reaction under the condition of having the general formula (III) of the aromatic amine compound; the second method: will have the general formula (I ‘) of the aromatic alcohol derivatives having the general formula (II) with the nitrogen containing compound mixed, in the acid additive and the presence of organic solvent prepared through the reaction of the formula (III) of the aromatic amine compound. The invention of the first use of the bulk of the alkyl aromatic compound or aromatic alcohol derivatives as raw materials, under the action of the non-metal catalytic, produced by the reaction of aromatic amine compound, compared with the traditional synthetic method with high yield, condition is simple, less waste emissions, does not need metal involved in, the reaction apparatus is simple, easy to industrial production and the like, therefore, has a wide application. (by machine translation)

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The synthesis of new polyheterocycles containing the pyrimido<2,1-a>phthalazine system 5, 6 and 7, obtained by condensation of phthalic anhydride with the appropriate hydrazides 2, 3 and 4, respectively, are reported.It was also synthesized the 14H-<1>Benzothieno<3',2':4,5>pyrimido<2,1-a><1,2,4>triazolo<4,3-c>phthalazin-14-one (16).

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Benzothiophene – Wikipedia,
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