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Efficient synthesis of a configurationally stable L-serinal derivative

An efficient synthesis of a configurationally stable L-serinal derivative 8 was achieved using an N-hydroxymethyl group in about 50% overall yield in four steps from L-serine. Not more than 1% racemization was observed during the preparation of 8. Its enantiomeric integrity was maintained for at least 15 days at room temperature, and it was stable on silica gel. The orthogonal protective groups of 8 would make it a useful chiral synthon.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Archives for Chemistry Experiments of Benzo[d]oxazol-2-amine

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Azolylthioacetamides as a potent scaffold for the development of metallo-beta-lactamase inhibitors

In an effort to develop new inhibitors of metallo-beta-lactamases (MbetaLs), twenty-eight azolylthioacetamides were synthesized and assayed against MbetaLs. The obtained benzimidazolyl and benzioxazolyl substituted 1?19 specifically inhibited the enzyme ImiS, and 10 was found to be the most potent inhibitor of ImiS with an IC50 value of 15 nM. The nitrobenzimidazolyl substituted 20?28 specifically inhibited NDM-1, with 27 being the most potent inhibitor with an IC50 value of 170 nM. Further studies with 10, 11, and 27 revealed a mixed inhibition mode with competitive and uncompetitive inhibition constants in a similar range as the IC50 values. These inhibitors resulted in a 2?4-fold decrease in imipenem MIC values using E. coli cells producing ImiS or NDM-1. While the source of uncompetitive (possibly allosteric) inhibition remains unclear, docking studies indicate that 10 and 11 may interact orthosterically with Zn2 in the active site of CphA, while 27 could bridge the two Zn(II) ions in the active site of NDM-1 via its nitro group.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Extended knowledge of 638192-65-1

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<1,4>Benzoxazine-2,3-diones as Antiallergic Agents

The synthesis of a series of <1,4>benzoxazine-2,3-diones and a new class of compounds, benzobisoxazinetetrones, is described.These compounds were evaluated for their effect in the rat mast cell (RMC) test passively sensitized in vitro with rat antiovalbumin serum and for their effect in inhibitory passive cutaneous anaphylaxis (PCA) in the rat.Some of this compounds are of the same potency level as disodium cromglycate in the RMC test and some are effective orally in PCA.

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Benzoxazole – Wikipedia,
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Final Thoughts on Chemistry for 5-Bromo-2-chlorobenzo[d]oxazole

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Related Products of 1030377-54-8, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 1030377-54-8, Name is 5-Bromo-2-chlorobenzo[d]oxazole, molecular formula is C7H3BrClNO. In a Patent£¬once mentioned of 1030377-54-8

COMPOUNDS USEFUL AS IMMUNOMODULATORS

The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Brief introduction of Benzo[d]oxazol-2-amine

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A Straightforward Access to [14C]- and [13C]-Labeled 2-Aminobenzoxazoles and Benzothiazoles via a KCN Polarity Inversion Strategy

A convenient one-pot synthetic access to 2-aminobenzoxazoles and 2-aminobenzothiazoles has been developed. The protocol uses KCN as starting material and proceeds through an in situ polarity inversion step. This approach provides a new valuable and straightforward entry to carbon-14-radiolabeled pharmaceutically relevant heterocycles and substantially reduces as well the amount of radioactive wastes generated.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Archives for Chemistry Experiments of Benzo[d]oxazole-5-carbaldehyde

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IL-8 RECEPTOR ANTAGONISTS

The invention relates to the use of guanidine compounds in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

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Benzoxazole – Wikipedia,
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Synthetic Route of 954239-61-3, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 954239-61-3, molcular formula is C9H6BrNO3, introducing its new discovery.

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,
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Electric Literature of 13451-79-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.13451-79-1, Name is 5-Fluorobenzo[d]oxazol-2(3H)-one, molecular formula is C7H4FNO2. In a Article£¬once mentioned of 13451-79-1

Iron-Catalyzed Arene C-H Amidation Using Functionalized Hydroxyl Amines at Room Temperature

Herein, we report Fe(III)(TPP)Cl as an effective catalyst for promoting arene C-H amidation through intramolecular cyclization of N-tosyloxyarylcarbamate substrates. The reaction proceeds via nitrene (outer sphere pathway) C(sp2)-H insertion to yield benzoxazolones under external-oxidant-free conditions at ambient temperature. The method is operationally simple and scalable with high-functional-group tolerance. Preliminary experimental and computational data indicates involvement of electrophilic aromatic substitution mechanism for this aryl C-H amidation transformation, distinct from operating mechanism reported previously in aryl C-H amination using azide-based substrates.

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Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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3,8-DIAZA-BICYCLO[4.2.0]OCT-8-YL AMIDES

The present invention relates to 3,8-diaza-bicyclo[4.2.0]oct-8-yl amide derivatives of formula (I) Formula (I) wherein the relative configuration of the diazabicyclooctane moiety is cis; and wherein Ar1, and Ar 2 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.

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Benzoxazole – Wikipedia,
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Reference of 64037-07-6, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.64037-07-6, Name is 5-Bromobenzo[d]oxazol-2-amine, molecular formula is C7H5BrN2O. In a Patent£¬once mentioned of 64037-07-6

COMBINATION OF KINASE INHIBITORS AND USES THEREOF

The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or a receptor tyrosine kinase (RTK) in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase alpha and/or an RTK in a subject. In yet another aspect, a method of inhibiting phosphorylation of Akt (S473) in a cell is set forth.

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Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem