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The present invention provides a tetrahydrofuran – 3 – preparation of method, comprising the addition of raw materials, amination reaction, hydrogenation reaction. In order to tetrahydrofuran – 3 – formaldehyde as raw materials, water as a reaction solvent, in under the action of the supported bimetallic catalyst, and the liquid ammonia in the amination reaction, inject the hydrogen reduction reaction to obtain the tetrahydrofuran – 3 – methylamine, high purity 99.8%, yield up to 99.1%. The invention of the tetrahydrofuran – 3 – preparation of method, with high yield, less catalyst levels, the operation is simple, low cost, and is suitable for industrial production. (by machine translation)

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The present application relates to cannabinoid receptor ligands containing compounds of formula (I)wherein A, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.

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Disclosed is an improved process for producing nitroguanidine derivatives represented by the following general formula (3), which has an insecticidal activity, or a salt thereof. Specifically, disclosed is a process for producing nitroguanidine derivatives represented by the following general formula (3) or a salt thereof, in which nitroisourea derivatives represented by the following general formula (1) or a salt thereof and compounds represented by the following general formula (2) or a salt thereof are reacted in the presence of a base in an aqueous solution wherein an inorganic salt is dissolved at not less than 50% of its saturated solubility, wherein, in the formula, R1 represents an alkyl group having 1 to 4 carbon atoms or a benzyl group; R2 represents an alkyl group having 1 to 4 carbon atoms; and R3 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, wherein, in the formula, R4, R5 and R6 each independently represent a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; and Q represents a 5- or 6-membered heterocyclic group which contains at least one each of a nitrogen atom, an oxygen atom and a sulfur atom and may be substituted with a halogen atom, wherein, in the formula, R2 represents an alkyl group having 1 to 4 carbon atoms; R3, R4, R5 and R6 each independently represent a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; and Q represents a 5- or 6-membered heterocyclic group which contains at least one each of a nitrogen atom, an oxygen atom and a sulfur atom and may be substituted with a halogen atom.

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The invention relates to a 3 – aminomethyl tetrahydrofuran preparation method, in particular the compound 1 maleric glycol through the cyclization to obtain compound 2 is 2, 5 – dihydrofuran, then a acylation to obtain compound 3 that 3 – formyl tetrahydrofuran, final reduction amination to obtain compound 4 that is 3 – aminomethyl tetrahydrofuran. The present invention production process is simple, the utilization rate of the material is high, the production capacity is large, each step catalyst has high selectivity, durability and high efficiency. By simple, easy industrialization the amplifying characteristic. (by machine translation)

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The invention relates to a 3 – aminomethyl tetrahydrofuran preparation method, in particular the compound 1 maleric glycol through the cyclization to obtain compound 2 is 2, 5 – dihydrofuran, then a acylation to obtain compound 3 that 3 – formyl tetrahydrofuran, final reduction amination to obtain compound 4 that is 3 – aminomethyl tetrahydrofuran. The present invention production process is simple, the utilization rate of the material is high, the production capacity is large, each step catalyst has high selectivity, durability and high efficiency. By simple, easy industrialization the amplifying characteristic. (by machine translation)

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A series of 2-pyridyl pyrimidines, reported inhibitors of Plasmodium falciparum methionine aminopeptidase 1b were synthesized and evaluated for their antiplasmodial activities. An analysis of physicochemical properties demonstrated a link between lipophilicity and antiparasitic activity. Cross screening of the library against cultured Leishmania donovani parasites revealed this class of compounds as potent inhibitors of parasite development in vitro.

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The invention discloses a 3 – aminomethyl tetrahydrofuran synthesis method, the method is: a, 1, 4 – butylene glycol in the fixed acid catalyst under the action of the condensation cyclization reaction to produce 2, 5 – dihydrofuran; b, 2, 5 dihydro furan in homogeneous catalyst HRhCO [P (PhX)3 ]3 Under the action of the, to carry out the hydroformylation reaction to obtain 3 – formaldehyde tetrahydrofuran; three, will be 3 – formaldehyde tetrahydrofuran with hydroxylamine compound reaction, to obtain 3 – a hydroxyimino tetrahydrofuran; four, the 3 – a hydroxyimino tetrahydrofuran under the action of catalyst to carry out hydrogenation reaction, to obtain 3 – aminomethyl tetrahydrofuran. Synthetic method of this invention simple process, steps is relatively short, the overall yield is very high, environmental protection, low cost, in each step of the product yield is greater than 90%, of the final prepared 3 – aminomethyl tetrahydrofuran overall yield is greater than 80%. (by machine translation)

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Substituted aromatic sulfonamides of formula (I) which are antagonists or negative allosteric modulators of P2X4, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease.

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Sirtuins (SIRTs) are NAD-dependent deacylases, known to be involved in a variety of pathophysiological processes and thus remain promising therapeutic targets for further validation. Previously, we reported a novel thienopyrimidinone SIRT2 inhibitor with good potency and excellent selectivity for SIRT2. Herein, we report an extensive SAR study of this chemical series and identify the key pharmacophoric elements and physiochemical properties that underpin the excellent activity observed. New analogues have been identified with submicromolar SIRT2 inhibtory activity and good to excellent SIRT2 subtype-selectivity. Importantly, we report a cocrystal structure of one of our compounds (29c) bound to SIRT2. This reveals our series to induce the formation of a previously reported selectivity pocket but to bind in an inverted fashion to what might be intuitively expected. We believe these findings will contribute significantly to an understanding of the mechanism of action of SIRT2 inhibitors and to the identification of refined, second generation inhibitors.

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Novel compounds of structural formula (I) are disclosed. As modulators of the Cannabinoid-1 (CB1) receptor, these compounds are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. As such, compounds of the present invention are useful as in the treatment, prevention and suppression of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders (e.g., multiple sclerosis, Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis), cerebral vascular accidents, head trauma, anxiety disorders, stress, epilepsy, Parkinson’s disease, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine. The compounds are also useful for the treatment of obesity or eating disorders associated with excessive food intake and complications associated therewith.

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