Category: 87392-07-2

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ABSOLUTE CONFIGURATIONS OF SOME HETEROCYCLIC ACIDS

Employing the method of asymmetric transformation, the absolute configurations of heterocyclic acids III, IV, Va, and VIIa have been determined.The acids Va and VIIa were chemically correlated with alcohols of known absolute configurations.

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

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INHIBITORS OF 11beta-HYDROXYSTEROID DEHYDROGENASE 1

This invention relates to novel compounds of the Formula (I), (Ia1-10), (Ib1-10), (Ic1-10), (Id1-7), (Ie1-5) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11beta-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.

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

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The most effective influence of 17-(3-ethoxypropyl) substituent on the binding affinity and the agonistic activity in KNT-127 derivatives, delta opioid receptor agonists

We investigated the structure-activity relationship of KNT-127 (opioid delta agonist) derivatives with various 17-substituents which are different in length and size. The 17-substituent in KNT-127 derivatives exerted a great influence on the affinity and agonistic activity for the delta receptor. While the compounds with electron-donating 17-substituents showed higher affinities for the delta receptor than those with electron-withdrawing groups, KNT-127 derivatives with 17-fluoroalkyl groups (the high electron-withdrawing groups) showed high selectivities for the delta receptor among evaluated compounds. In addition, the basicity of nitrogen as well as the structure of the 17-N substituent such as the length and configuration at an asymmetric carbon atom contributed to agonist properties for the delta receptor. Thus, the analog with a 17-(3-ethoxypropyl) group showed the best selectively and potent agonistic activity for the delta receptor among KNT-127 derivatives. These findings should be useful for designing novel delta selective agonists.

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

87392-07-2, Name is (S)-Tetrahydrofuran-2-carboxylic acid, belongs to tetrahydrofurans compound, is a common compound. Quality Control of (S)-Tetrahydrofuran-2-carboxylic acidIn an article, once mentioned the new application about 87392-07-2.

Nucleotide competing reverse transcriptase inhibitors: Discovery of a series of non-basic benzofurano[3,2-d]pyrimidin-2-one derived inhibitors

A HTS screen led to the identification of a benzofurano[3,2-d]pyrimidin-2- one core structure which upon further optimization resulted in 1 as a potent HIV-1 nucleotide competing reverse transcriptase inhibitor (NcRTI). Investigation of the SAR at N-1 allowed significant improvements in potency and when combined with the incorporation of heterocycles at C-8 resulted in potent analogues not requiring a basic amine to achieve antiviral activity. Additional modifications at N-1 resulted in 33 which demonstrated excellent antiviral potency and improved physicochemical properties.

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

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BICYCLIC COMPOUNDS AS MPGES-1 INHIBITORS

The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 87392-07-2 is helpful to your research. Related Products of 87392-07-2

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

Reference of 87392-07-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.87392-07-2, Name is (S)-Tetrahydrofuran-2-carboxylic acid, molecular formula is C5H8O3. In a Article，once mentioned of 87392-07-2

Rubrosides A-H, new bioactive tetramic acid glycosides from the marine sponge Siliquariaspongia japonica

Eight new tetramic acid glycosides named rubrosides A-H have been isolated from the marine sponge Siliquariaspongia japonica. Their structures were elucidated on the basis of spectral data as tetramic acid glycosides containing polyenes terminating in a 4-chloro-2-methyltetrahydrofuran ring. The absolute stereochemistry of the furan functionality in the two major metabolites, rubrosides D and F, was determined by the NMR method using chiral anisotropic reagents for tetrahydro-2-furoic acid derived by RuO4 oxidation. The absolute stereochemistry of tetramic acid and of the sugar moieties in all rubrosides was deduced by chiral GC analysis of chemical degradation products. The rubrosides induced numerous large intracellular vacuoles in 3Y1 rat fibroblasts at concentrations of 0.5-1.0 mug/mL, and rubrosides A, C, D, and E were cytotoxic against P388 murine leukemia cells with IC50 values of 0.046-0.21 mug/mL. Most rubrosides show antifungal activity against Aspergillus fumigatus and Candida albicans.

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

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A high-optical-purity 1 – [tetrahydro-2-furyl] ethanone industrial preparation method (by machine translation)

The invention discloses a high-optical-purity 1 – [tetrahydro-2-furyl] ethanone industrial preparation method, belongs to the field of chemical synthesis, comprising the following steps: with tetrafuran formic acid as the raw material, reaction with carbonyl diimidazole, then adding malonic acid asian different propyl ester for condensation, then hydrolyzed in acidic conditions, the final extraction, concentrated to obtain product acetylprotoaescigenin tetrahydrofuran; the invention to prepare the high-optical-purity 1 – [tetrahydro-2-furyl] ethanone process, low cost of raw materials, do not need to use the Grignard reagent, stable product characteristics, the purity can be up to 98% or more, the optical purity can be up to 99% or more, the yield can reach 70% or more; the process after the actual commercial production verification, the quality is stable, mild reaction conditions, the operation is safe and reliable, process repeatability is good, the production cost is low, is a reliable high-optical-purity 1 – [tetrahydro-2-furyl] ethanone industrial preparation method. (by machine translation)

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

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Carboxylic acids as A traceless activation group for conjugate additions: A three-step synthesis of (¡À)-pregabalin

The direct application of carboxylic acids as a traceless activation group for radical Michael additions has been accomplished via visible light-mediated photoredox catalysis. Photon-induced oxidation of a broad series of carboxylic acids, including hydrocarbon-substituted, alpha-oxy, and alpha-amino acids, provides a versatile CO2-extrusion platform to generate Michael donors without the requirement for organometallic activation or propagation. A diverse array of Michael acceptors is amenable to this new conjugate addition strategy. An application of this technology to a three-step synthesis of the medicinal agent pregabalin (commercialized by Pfizer under the trade name Lyrica) is also presented.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Application of 87392-07-2. In my other articles, you can also check out more blogs about 87392-07-2

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

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Hepatitis C virus NS5A replication complex inhibitors: The discovery of daclatasvir

The biphenyl derivatives 2 and 3 are prototypes of a novel class of NS5A replication complex inhibitors that demonstrate high inhibitory potency toward a panel of clinically relevant HCV strains encompassing genotypes 1-6. However, these compounds exhibit poor systemic exposure in rat pharmacokinetic studies after oral dosing. The structure-activity relationship investigations that improved the exposure properties of the parent bis-phenylimidazole chemotype, culminating in the identification of the highly potent NS5A replication complex inhibitor daclatasvir (33) are described. An element critical to success was the realization that the arylglycine cap of 2 could be replaced with an alkylglycine derivative and still maintain the high inhibitory potency of the series if accompanied with a stereoinversion, a finding that enabled a rapid optimization of exposure properties. Compound 33 had EC50 values of 50 and 9 pM toward genotype-1a and -1b replicons, respectively, and oral bioavailabilities of 38-108% in preclinical species. Compound 33 provided clinical proof-of-concept for the NS5A replication complex inhibitor class, and regulatory approval to market it with the NS3/4A protease inhibitor asunaprevir for the treatment of HCV genotype-1b infection has recently been sought in Japan.

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

Chemistry is traditionally divided into organic and inorganic chemistry. HPLC of Formula: C5H8O3, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 87392-07-2

4-AMINO-BENZAMIDE DERIVATIVES AS 5-HT4 RECEPTOR AGONISTS FOR THE TREATMENT OF GASTROINTESTINAL, NEUROLOGICAL AND CARDIOVASCULAR DISORDERS

The present invention relates to novel benzamide derivatives of formula (I) having pharmacological activity, to processes for their preparation, to compositions containing them and to their use in the treatment of diseases treatable by 5-HT4 agonism.

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