Category: 87392-05-0

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NOVEL DIHYDROPYRIDINONE AND DIHYDROPYRIMIDINONE COMPOUNDS AND THEIR USE

The present invention is directed to novel compounds of Formula I; pharmaceutically acceptable salts or solvates thereof, and their use.

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

87392-05-0, Name is (R)-(+)-2-Tetrahydrofuroic acid, belongs to tetrahydrofurans compound, is a common compound. Safety of (R)-(+)-2-Tetrahydrofuroic acidIn an article, once mentioned the new application about 87392-05-0.

LINKED DIBENZIMIDAZOLE DERIVATIVES

The present invention discloses linked dibenzimidazole derivatives, or pharmaceutically acceptable salts, esters, or prodrugs thereof, which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

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

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SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS

Provided herein are compounds of the General Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.

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

Synthetic Route of 87392-05-0, 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. 87392-05-0, Name is (R)-(+)-2-Tetrahydrofuroic acid, molecular formula is C5H8O3. In a Article，once mentioned of 87392-05-0

Regio- and stereoselective Pd-catalyzed direct arylation of unactivated sp3 C(3)-H bonds of tetrahydrofuran and 1,4-benzodioxane systems

An auxiliary-enabled Pd-catalyzed highly regio- and stereoselective sp3 C-H activation and the direct arylation of the C3-position of oxygen heterocycles, such as tetrahydrofuran and 1,4-benzodioxane systems, are reported. An efficient stereoselective construction of cis 2,3-disubstituted tetrahydrofuran derivatives (analogues of norlignans) and cis 2,3-disubstituted 1,4-benzodioxane derivatives (analogues of neolignans) is described. The direct C(sp3)-H arylation of the C3-position of (R)- or (S)- tetrahydrofuran-2-carboxamides furnished the corresponding (2R,3R) and (2S,3S) C3-arylated THF scaffolds as major compounds with very high regio- and diastereoselectivities. The stereochemistry of the products obtained in this work were unambiguously assigned on the basis of the X-ray structure analyses of representative compounds 3b, 3e, 4p, and 7.

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

87392-05-0, Name is (R)-(+)-2-Tetrahydrofuroic acid, belongs to tetrahydrofurans compound, is a common compound. Recommanded Product: (R)-(+)-2-Tetrahydrofuroic acidIn an article, once mentioned the new application about 87392-05-0.

Design and synthesis of potent, orally efficacious hydroxyethylamine derived beta-Site amyloid precursor protein cleaving enzyme (Bace1) inhibitors

We have previously shown that hydroxyethylamines can be potent inhibitors of the BACE1 enzyme and that the generation of BACE1 inhibitors with CYP 3A4 inhibitory activities in this scaffold affords compounds (e.g., 1) with sufficient bioavailability and pharmacokinetic profiles to reduce central amyloid-beta peptide (Abeta) levels in wild-type rats following oral dosing. In this article, we describe further modifications of the P1-phenyl ring of the hydroxyethylamine series to afford potent, dual BACE1/CYP 3A4 inhibitors which demonstrate improved penetration into the CNS. Several of these compounds caused robust reduction of Abeta levels in rat CSF and brain following oral dosing, and compound 37 exhibited an improved cardiovascular safety profile relative to 1.

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

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, COA of Formula: C5H8O3, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 87392-05-0, Name is (R)-(+)-2-Tetrahydrofuroic acid, molecular formula is C5H8O3

SYNTHESIS OF TRANS-TERT-BUTYL-2-AMINOCYCLOPENTYLCARBAMATE

The present invention concerns methods of synthesis of trans-tert-butyl-2- aminocylcopentylcarbamate comprising contacting 6-tosyl-6-azabicyclo[3.1.0]hexane with TMSN3 and TBAF to produce 2-azido-N-tosylcyclopentananiine; reducing the 2- azido-N-tosylcyclopentanamine to produce 2-amino-N-tosylcyclorhoentanamine; contacting the 2-amino-N-tosylcyclopentanamine with di-tert/-butyl dicarbonate to produce tert-butyl- 2-(tosylamino)cyclopentylcarbamate; and detosylation of tert-butyl (tosylamino) cyclopentylcarbamate to produce trans-tert-butyl-2-aminocyclopentylcarbamate. The invention also concerns PNAs comprising residues of the monomers of the invention in the backbone and uses of such PNAs. The PNAs of the invention can be used to detect DNAs of infectious agents or to suppress expression of protein associated with cancer.

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

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 87392-05-0, name is (R)-(+)-2-Tetrahydrofuroic acid, introducing its new discovery. Quality Control of (R)-(+)-2-Tetrahydrofuroic acid

Synthesis, Structure, and Pharmacological Evaluation of the Stereoisomers of Furnidipine

The synthesis and pharmacological activities of the four stereoisomers of methyl tetrahydrofuran-2-ylmethyl 2,6-dimethyl-4-(2′-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate (furnidipine) are reported.The four isomers were synthesized by a modified Hantzsch synthesis by reaction of (-)- or (+)-tetrahydrofuran-2-ylmethyl 3-aminocrotonate and methyl 2-<(2'-nitrophenyl)methylene>acetoacetate or, alternatively, by reaction of (-)- or (+)-tetrahydrofuran-2-ylmethyl 2-<(2'-nitrophenyl)methylene>acetoacetate and methyl 3-aminocrotonate.The 1:1 diasteromeric mixture thus obtained were separated by chromatography, using poly(D-phenylglycine) as the chiral stationary phase.The enantiomeric purity of the stereoisomers was determined by high-performance liquid chromatography-chiral stationary phase technique (HPLC-CSP).Attempts to obtain crystals of a single stereoisomer failed in different solvent, while methanol crystallization of the product obtained from (+/-)-tetrahydrofuran-2-ylmethyl 2-<(2'-nitrophenyl)methylene>acetoacetate and methyl 3-aminocrotonate yielded good-quality crystals of the most insoluble racemate which proved to be a mixture of the (SS)/(RR) enantiomers by X-ray crystaloography.Conformational analysis of the stereoisomers, assuming rotation of the aryl substituent and ester groups, shows small energy differences (about 4 kcal*mol-1) between the most and the least favorable conformations.Binding studies were performed using <3H>isradipine as a reference ligand.The results showed stereospecificity of the furnidipine isomers in brain, ileum, and cardiac tissues, the (SS) and (SR)-isomers clearly being more potent than their (RR)- and (RS)-enantiomers.The (SS)- and (SR)-isomers were also more selective on cerebral tissue when compared with ileal and cardiac preparations.

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

Chemistry is traditionally divided into organic and inorganic chemistry. Safety of (R)-(+)-2-Tetrahydrofuroic acid, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent，Which mentioned a new discovery about 87392-05-0

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

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, name: (R)-(+)-2-Tetrahydrofuroic acid, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 87392-05-0, Name is (R)-(+)-2-Tetrahydrofuroic acid, molecular formula is C5H8O3

Synthesis and Chromatographic Separation of the Stereoisomers of Furnidipine

The four stereoisomers of methyl tetrahydrofuran-2-ylmethyl 2,6-dimethyl-4-(o-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate (furnidipine), have been synthesized and separated by chiral chromatography using D-phenylglycine as chiral stationary phase.Enantiomeric purity of stereoisomers is determined by HPLC-CSP technique and configurations deduced via X-ray crystallography.

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

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Application In Synthesis of (R)-(+)-2-Tetrahydrofuroic acid, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 87392-05-0, Name is (R)-(+)-2-Tetrahydrofuroic acid, molecular formula is C5H8O3

Asymmetric cycloetherification based on a chiral auxiliary for 4-acyloxy-1-butene substrates during oxidation with iodosylbenzene via a 1,3-dioxan-2-yl cation

Reaction of but-3-enyl camphanate and its derivatives with iodosylbenzene yielded tetrahydrofuran-3-yl camphanate with high diastereomeric ratio via a 1,3-dioxan-2-yl cation intermediate. The reaction using (1S)-camphanate as a chiral auxiliary preferentially gave (S)-3-acyloxytetrahydrofuran and (2S,3S)-3-acyloxy-2-silyltetrahydrofuran.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Application In Synthesis of (R)-(+)-2-Tetrahydrofuroic acid, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 87392-05-0, in my other articles.

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