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FUNGICIDAL AMINES

Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein R1, R2, R9a, R9b, G, W, X, Y, and Z are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (1) and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.

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Lewis Acid Catalyzed Electrophilic Aminomethyloxygenative Cyclization of Alkynols with N, O-Aminals

Lewis acid enables the electrophilic carbooxygenative cyclization of alkynols with N,O-aminals. The new process proceeds efficiently under very mild conditions via a pathway that is opposite to classical carbo-metalation. These reactions exhibit broad substrate generality and functional group compatibility, leading to a wide variety of 5-8-membered oxacycles bearing diverse functional groups. The cyclization products can be elaborated via simple functional group transformations to generate synthetically useful oxacycles.

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. COA of Formula: C5H11NO, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 165253-31-6, name is (Tetrahydrofuran-3-yl)methanamine. In an article£¬Which mentioned a new discovery about 165253-31-6

INDOLINE DERIVATIVES

The present invention provides a novel indoline derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or a salt thereof represented by the following formula (1) that has an excellent butyrylcholinesterase inhibitory activity. In the formula, R1 represents an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, a hetero aryl group, an arylalkyl group, a heteroarylalkyl group, a cycloalkylalkyl group, a heterocycloalkylalkyl group, a dihydrofurylalkyl group, an alkenyl group, a tetrahydronaphthyl group, or an indanyl group; R2 represents a hydrogen atom, an alkyl group, an arylalkyl group, a cycloalkylalkyl group, a heteroarylalkyl group, a heterocycloalkylalkyl group, an aryl group, or an acyl group; R3 each independently represents a hydrogen atom, an alkyl group, or a dialkylaminocarbonyl group; R4 each independently represents a hydrogen atom or an alkyl group; and R5 represents a hydrogen atom or an alkyl group. Each functional group may have a substituent.

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Extracurricular laboratory:new discovery of (Tetrahydrofuran-3-yl)methanamine

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A dinotefuran intermediate 3 – amino methyl tetrahydrofuran preparation method (by machine translation)

The invention relates to a kind of dinotefuran intermediate 3 – amino methyl tetrahydrofuran preparation method, specifically it is to cyano acetic acid ester as the raw material, first with 1, 2 – dihalo ethane condensation reaction to obtain the intermediate 2 – halogenated ethyl – 2 – cyano – acetate, followed by a further reduction to obtain intermediate 2 – halogenated ethyl – 2 – cyano – ethanol, then intermediate 2 – halogenated ethyl – 2 – cyano – ethanol cyclization to obtain intermediate 3 – cyano tetrahydrofuran; the final 3 – cyano tetrahydrofuran obtained by catalytic hydrogenation of dinotefuran intermediate 3 – amino methyl tetrahydrofuran. Preparation method of the invention, raw materials are easy, simple operation, low production cost, and thus is suitable for industrial production. (by machine translation)

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A 2 – nitro – 1, 3 – b [(tetrahydro -3 – furan) methyl] guanidine synthetic preparation method (by machine translation)

The present invention provides a 2 – nitro – 1, 3 – b [(tetrahydro – 3 – furyl) methyl] guanidine synthetic preparation method, in particular relates to a technical field of chemical synthesis, the (tetrahydro – 3 – furan) methylamine and O – methyl – N – nitro-isourea in saturated sodium chloride aqueous solution in the reaction, finally the resulting oily product is purified, by preparative high performance liquid chromatography separation and purification, to obtain 2 – nitro – 1, 3 – b [(tetrahydro – 3 – furyl) methyl] guanidine of the pure substance. The invention after HPLC – MS and 1 H NMR and 13 C NMR confirmation, purity of about 99.0%, thus can be applied to the report of the related impurities of GLP in qualitative and quantitative and economically feasible, the operation is simple, the universality is relatively strong, the yield is high. (by machine translation)

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FORMYLATED N-HETEROCYCLIC DERIVATIVES AS FGFR4 INHIBITORS

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; (I) a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

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Top Picks: new discover of (Tetrahydrofuran-3-yl)methanamine

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Thiazolopyridine ureas as novel antitubercular agents acting through inhibition of DNA gyrase B

A pharmacophore-based search led to the identification of thiazolopyridine ureas as a novel scaffold with antitubercular activity acting through inhibition of DNA Gyrase B (GyrB) ATPase. Evaluation of the binding mode of thiazolopyridines in a Mycobacterium tuberculosis (Mtb) GyrB homology model prompted exploration of the side chains at the thiazolopyridine ring C-5 position to access the ribose/solvent pocket. Potent compounds with GyrB IC 50 ? 1 nM and Mtb MIC ? 0.1 muM were obtained with certain combinations of side chains at the C-5 position and heterocycles at the C-6 position of the thiazolopyridine core. Substitutions at C-5 also enabled optimization of the physicochemical properties. Representative compounds were cocrystallized with Streptococcus pneumoniae (Spn) ParE; these confirmed the binding modes predicted by the homology model. The target link to GyrB was confirmed by genetic mapping of the mutations conferring resistance to thiazolopyridine ureas. The compounds are bactericidal in vitro and efficacious in vivo in an acute murine model of tuberculosis.

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SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT)

Herein we disclose SAR studies that led to a series of isoindoline ureas which we recently reported were first-in-class, non-substrate nicotinamide phosphoribosyltransferase (NAMPT) inhibitors. Modification of the isoindoline and/or the terminal functionality of screening hit 5 provided inhibitors such as 52 and 58 with nanomolar antiproliferative activity and preclinical pharmacokinetics properties which enabled potent antitumor activity when dosed orally in mouse xenograft models. X-ray crystal structures of two inhibitors bound in the NAMPT active-site are discussed.

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Preparation method of 3- aminomethyltetrahydrofuran (by machine translation)

The method disclosed by the 3 – invention is low in cost, easy and simple to operate, low, in cost and low 3 – in cost, 3 . (by machine translation)

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MICROBIOCIDAL OXADIAZOLE DERIVATIVES

Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides, especially as fungicides.

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