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Copper-catalyzed oxidative decarboxylative C-H arylation of benzoxazoles with 2-nitrobenzoic acids

A copper-catalyzed oxidative decarboxylative coupling of benzoxazoles with 2-nitrobenzoic acids was developed. This methodology favors electron-rich benzoxazoles and electron-deficient benzoic acids and enables the preparation of a variety of arylated benzoxazoles in good yields. The trends in product yields suggest a delicate balance between the decarboxylation and C-H arylation steps.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Cobalt-Catalyzed Decarboxylative 2-Benzoylation of Oxazoles and Thiazoles with alpha-Oxocarboxylic Acids

Cobalt-catalyzed decarboxylative cross-coupling of oxazoles and thiazoles with alpha-oxocarboxylic acids was developed through an sp2 C-H bond functionalization process. This work represents the first example of cobalt-catalyzed decarboxylative C-H bond functionalization and provides an efficient means of building some important bioactive heteroaryl ketone derivatives.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Structure-activity relationships of phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: Investigations of various 6,5-heterocycles to improve metabolic stability

N-(6-(6-Chloro-5-(4-fluorophenylsulfonamido)pyridin-3-yl)benzo[d] thiazol-2-yl)acetamide (1) is a potent and efficacious inhibitor of PI3Kalpha and mTOR in vitro and in vivo. However, in hepatocyte and in vivo metabolism studies, 1 was found to undergo deacetylation on the 2-amino substituent of the benzothiazole. As an approach to reduce or eliminate this metabolic deacetylation, a variety of 6,5-heterocyclic analogues were examined as an alternative to the benzothiazole ring. Imidazopyridazine 10 was found to have similar in vitro potency and in vivo efficacy relative to 1, while only minimal amounts of the corresponding deacetylated metabolite of 10 were observed in hepatocytes.

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Benzoxazole – Wikipedia,
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Copper-Catalyzed Three-Component Carboamination of Arynes: Expeditious Synthesis of o-Alkynyl Anilines and o-Benzoxazolyl Anilines

A copper-catalyzed three-component reaction of in situ formed arynes, terminal alkynes, and O-benzoylhydroxylamines has been developed. By adjusting reaction conditions, the nucleophiles in this transformation can be extended from terminal alkynes to benzoxazoles. These procedures provide a modular and facile approach to o-alkynyl anilines and o-benzoxazolyl anilines from easily available substrates in only one step.

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Benzoxazole – Wikipedia,
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PI3 KINASE MODULATORS AND METHODS OF USE

The present invention comprises a new class of compounds capable of modulating the activity of PI3 kinase and, accordingly, useful for treatment of PI3 kinase mediated diseases, including melanomas, carcinomas and other cancer-related conditions. The compounds have a general Formula I wherein each of A1, A2, A3, A4, X, R1 and R2 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of PI3 kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Binuclear molybdenum alkoxide as the versatile catalyst for the conversion of carbon dioxide

The triply bonded dimolybdenum compound, Mo2(OtBu)6 (1), was investigated as a homogeneous catalyst for the conversion of CO2. The compound 1 acted as a rare example of a versatile catalyst with an impressive ability to transform CO2 into various valuable products, including propiolic acids, cyclic carbonates, and benzo[d]thiazole- and benzo[d]oxazolecarboxylic acids, in high yields with short reaction times and excellent selectivity at ambient pressure and low temperatures (25-75 C). This is the first report of the application of a metal-metal bond-containing species in the catalytic conversion of CO2.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Ytterbium(III) Trifluoromethanesulfonate Catalyzed Ring-Opening C(sp3)?N Bond Formation of Benzoxazoles with Propargylic Alcohols

A novel ytterbium(III) trifluoromethanesulfonate [Yb(OTf)3]-catalyzed ring-opening C(sp3)?N bond formation reaction of benzoxazole with propargylic alcohols was established. This reaction uses readily available starting materials and is operationally simple; it thus represents a practical method for the construction of highly functionalized substituted benzenes bearing aldehyde, propargylamine, and hydroxy groups with high atom economy.

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BENZIMIDAZOLES AS FATTY ACID SYNTHASE INHIBITORS

This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of benzimidazoles in the treatment of cancer.

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CuCl-Catalyzed direct C-H alkenylation of benzoxazoles with allyl halides

An efficient and concise CuCl-catalyzed C2-alkenylation reaction of benzoxazoles with allyl halides has been established. The distinctive features of this protocol include the use of an inexpensive copper salt as a catalyst, simple and readily available starting materials, and ligand-free conditions. An important application of this method to the synthesis of 1,3-diene substituted benzoxazoles has also been achieved.

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A microwave radiation in the aqueous phase benzamide compound synthesis benzoxazole method (by machine translation)

The invention discloses a microwave radiation in the aqueous phase benzamide compound synthesis benzoxazole method, in the aqueous phase under microwave conditions to join the benzamide compound under alkaline condition […] benzene and oxazole reaction, invention an environment-friendly, the operation is simple, cheap and safe, efficient preparation BENZOXAZOL method. Compared with the prior art, this method not only can be applied to a large number of functional groups, the productive rate is high, few by-products, and the operation is simple, safe, low cost, environmental protection; . (by machine translation)

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Benzoxazole – Wikipedia,
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