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Design, Synthesis, and Antimicrobial Activity of Novel 6-Oxopyrimidin-1(6H)-yl Benzamide Derivatives

A series of novel 1-(benzamide)-N-cyclopropyl-2-(amino substituted)-6-oxo-1,6-dihydropyrimidine-5-carboxamide derivatives is synthesised and characterized by IR, 1H and 13C NMR, and mass spectra. The synthesized compounds 6a-6j and 8a-8j are screened for their in vitro antimicrobial activity against two Grampositive (Staphylococcus aureus, Bacillus subtilis) and two Gram-negative bacteria (Escherichia coli, Klebesiella aerogenes), and two pathogenic fungi (Aspergillus flavus, Fusarium oxysporum). Most of the compounds demonstrate good to excellent antimicrobial activity in comparison with the standard drugs ciproflaxin and hymexazole. Among the screened compounds morpholine substituted dihydropyrimidone carboxamide 8j is determined to be the most potent anti-bacterial agent.

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Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Preparation of amines

Disclosed is a process for the preparation of an amine by contacting in a reaction zone a water-soluble aldehyde, water, ammonia and hydrogen in the presence of a supported ruthenium catalyst at elevated temperature and pressure. The process is particularly useful for the preparation of 3-(aminomethyl)tetrahydrofuran by contacting an aqueous solution of 3-formyltetrahydrofuran with ammonia and hydrogen at elevated temperature and pressure in the presence of a supported ruthenium catalyst. The use of a supported ruthenium catalyst has been found to avoid the problem of catalyst leaching encountered when a nickel catalyst is used.

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Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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A tetrahydrofuran – 3 – methylamine novel synthesis process (by machine translation)

The invention discloses a tetrahydrofuran – 3 – methylamine novel synthesis process, solved in the prior art in a manufacturing process, the raw materials are not only expensive, raising the production cost, but also the production process would release a large amount of heat and flammable and explosive gas hydrogen, will be brought to the production the security risk. The invention comprises (1) in the organic solvent, 2, 5 – dihydrofuran catalyst under the action of the A poly formaldehyde and hydrogen chloride reaction, to obtain the methyl – 2, 5 – dihydrofuran; (2) methyl – 2, 5 – dihydrofuran with hexamine reaction to obtain the amine methyl – 2, 5 – dihydro benzofuran hydrochloride, then using sodium hydroxide solution free leaves the amine methyl – 2, 5 – dihydrofuran, distilled to obtain crude; (3) the crude amine methyl – 2, 5 – dihydrofurans under the effects of catalyst by the hydrogen reduction to obtain 3 – tetrahydrofuran methylamine, filtering, rectifying the filtrate to obtain the pure product. The invention has the low cost of raw materials, little three-waste discharge, simple process and the like. (by machine translation)

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Tetrahydrofuran – Wikipedia,
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Expansion of the structure-activity relationships of BACE1 inhibitors by harnessing diverse building blocks prepared using a unified synthetic approach

The structural diversity of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors was expanded by harnessing diverse building blocks that had been prepared via a unified lead-oriented synthetic approach. It was shown that the lipophilic cyclohexylmethyl group within a known series of BACE1 inhibitors could be productively replaced with a range of alternative ring systems.

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Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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HETEROCYCLIC COMPOUND

Provided is a heterocyclic compound that may have a GCN2 inhibitory action, and is expected to be useful for the prophylaxis or treatment of GCN2 associated diseases including cancer and the like. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof.

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Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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INHIBITORS OF JANUS KINASES

The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.

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Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Furanyl insecticide

The present invention relates to novel (tetrahydro-3-furanyl)methylamino derivatives of the following formula (1): STR1 wherein the variables are defined in the specification, which are useful as insecticides.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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

The invention relates to a 3 – amino-methyl-tetrahydrofuran of the preparation method. Specifically involves the reduction 3 – cyano tetrahydrofuran preparation 3 – amino methyl tetrahydrofuran. This invention adopts a new synthetic process, namely in order to gamma – butyrolactone and halogen simple substance X2 As the raw material to prepare the 3 – X – gamma – butyrolactone, then use the reducing agent 3 – X – gamma – butyrolactone obtained 2 – X – 1, 4 – butanediol, then under the action of a dehydrating agent to obtain 3 – X tetrahydrofuran, and under the action of the hydrocyanation catalyst to obtain 3 – cyano tetrahydrofuran, finally the hydrogenation catalyst obtained under the action of the 3 – amino methyl four hydrogen fu. This synthetic process raw materials are easy, simple experimental operation, mild reaction conditions, product yield and purity are relatively high, small pollution to the environment, the production cost is low, and is suitable for industrial expansion of production, very broad application prospect. (by machine translation)

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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A 3 – amino methyl tetrahydrofuran synthetic method (by machine translation)

The invention relates to a 3 – amino methyl tetrahydrofuran synthetic method. The method in order to 2, 5 – dihydrofuran as the starting material, by catalytic hydroformylation of Rh and catalytic reduction ammoniation two-step reaction synthesis of 3 – amino methyl tetrahydrofuran. Synthesis method of the invention the reaction selectivity is high, simple process operation, short synthetic route, the two-step yield of the reaction can be up to 95% or more, is suitable for industrial production. (by machine translation)

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Tetrahydrofuran – Wikipedia,
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A synthetic method of the dinotefuran (by machine translation)

The invention discloses a method for synthesis of dinotefuran, to gamma – butyrolactone as raw materials, by Aldol condensation, also the original two-step by the reaction of 3 – hydroxy methyl tetrahydrofuran, then by the Gabriel synthesis of 3 – tetrahydrofuran methyl amine, dimethyl carbonate (DMC) as methylation reagent with the urea synthesis O – methyl isourea, re-nitration synthetic O – methyl – N – nitro-isourea, then with the methylamine reaction synthesis of 1, 3 – dimethyl – 2 – nitro-isourea, final 3 – tetrahydrofuran methylamine with 1, 3 – dimethyl – 2 – nitro-isourea through SN2 Bimolecular nucleophilic substitution reaction, one-step synthesis of dinotefuran. The present invention uses non of dimethyl carbonate as the methylating reagent, the methylation reaction yield ? 95%, O – methyl isourea content ? 96%, the by-product is carbon dioxide and methanol, process and environmental protection, the overall yield of the dinotefuran ? 50%. Synthetic method of this invention to reduce the production cost at the same time, with three wastes, after treatment is simple, the advantages of the environment friendly, and is suitable for industrial production, bring about significant economic benefits. (by machine translation)

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Reference£º
Tetrahydrofuran – Wikipedia,
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