The important role of 3-Hydroxytetrahydrofuran

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Structural identification of binary tetrahydrofuran + O2 and 3-hydroxytetrahydrofuran + O2 clathrate hydrates by rietveld analysis with direct space method

The structural determination of clathrate hydrates, nonstoichiometric crystalline host-guest materials, is challenging because of the dynamical disorder and partial cage occupancies of the guest molecules. The application of direct space methods with Rietveld analysis can determine the powder X-ray diffraction (PXRD) patterns of clathrates. Here, we conducted Rietveld analysis with the direct space method for the structural determination of binary tetrahydrofuran (THF) + O2 and 3-hydroxytetrahydrofuran (3-OH THF) + O2 clathrate hydrates in order to identify the hydroxyl substituent effect on interactions between the host framework and the cyclic ether guest molecules. The refined PXRD results reveal that the hydroxyl groups are hydrogen-bonded to host hexagonal rings of water molecules in the 512 64 cage, while any evidences of hydrogen bonding between THF guests and the host framework were not observed from PXRD at 100 K. This guest-host hydrogen bonding is thought to induce slightly larger 512 cages in the 3-OH THF hydrate than those in the THF hydrate. Consequently, the disorder dynamics of the secondary guest molecules also can be affected by the hydrogen bonding of larger guest molecules. The structural information of binary clathrate hydrates reported here can improve the understanding of the host-guest interactions occurring in clathrate hydrates and the specialized methodologies for crystal structure determination of clathrate hydrates.

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

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BMP-SIGNAL-INHIBITING COMPOUND

The present invention relates to novel and excellent small-molecule-corn pounds that specifically antagonize BMP signal pathways, and these compounds can be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus can be used to treat diseases or pathological symptoms related to BMP signal pathway including inflammation, cardiovascular diseases, hematopoietic diseases, cancer, osteodystrophia, or the like, particularly, fibrodysplasia ossificans progressiva, and the present invention relates to provision of a pharmaceutical and pharmacological agent used for specifically antagonizing the BMP signal pathways and acting on the BMP signal pathways in the prevention and treatment or experimental application since the compounds can be beneficial for regulating cell differentiation and/or cell proliferation.

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

Simple exploration of 3-Hydroxytetrahydrofuran

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Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A1receptor antagonists and their biological evaluation

Multipronged approach was used to synthesize a library of diverse C-8 cyclopentyl hypoxanthine analogs from a common intermediate III. Several potent and selective compounds were identified and evaluated for pharmacokinetic (PK) properties in Wistar rats. One of the compounds 14 with acceptable PK parameters was selected for testing in in vivo primary acute diuresis model. The compound demonstrated significant diuretic activity in this model.

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

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Mild deprotection of PMB ethers using tert-butyl bromide

A convenient and high yielding method for the cleavage and scavenging of p-methoxybenzyl protecting group of several alcohols using tert-butyl bromide in refluxing acetonitrile is described. Under these mild conditions other protecting groups such as acid sensitive allyl, benzyl, and Me3CPh2Si ethers, or isopropylidene acetals were unchanged. Interestingly, a selective alkoxy-PMB cleavage was observed in the presence of a PMB phenoxy ether.

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

Brief introduction of 453-20-3

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Cephalosporin derivatives

A new class of cephalosporin derivatives is provided, which is useful as antibacterial agent to be particularly suitable for oral administrations in mammals including man, and which is represented by general formula (I) STR1 wherein R1 is a hydrogen atom or a lower alkyl group; R2 is a hydrogen atom or an ester-forming group capable of being cleaved easily with an esterase existing in the digestive tracts; n is an integer of zero or 1; Z is a saturated heterocyclic group containing one or two oxygen atoms as the hetero-atoms with or without one or more lower alkyl substituents, or a pharmaceutically acceptable salt thereof.

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

Discovery of 453-20-3

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PROTEIN TYROSINE KINASE MODULATORS AND METHODS OF USE

Heterocyclic pyrimidine compounds that modulate mutant-selective epidermal growth factor receptor (EGFR) and ALK kinase activity are disclosed. More specifically, the invention provides pyrimidines which inhibit, regulate and/or modulate kinase receptor, particularly in selectively modulation of various EGFR mutant activity and ALK kinase activity have been disclosed. Pharmaceutical compositions comprising the pyrimidine derivative,and methods of treatment for diseases associated with protein kinase enzymatic activity, particularly EGFR or ALK kinase activity including non-small cell lung cancer comprising administration of the pyrimidine derivative are disclosed.

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

The Absolute Best Science Experiment for 453-20-3

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NEW HETEROCYCLIC AMIDES

The present invention relates to new compounds (I) or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.

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

Some scientific research about 453-20-3

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Synthesis and SAR studies of novel 1,2,4-oxadiazole-sulfonamide based compounds as potential anticancer agents for colorectal cancer therapy

A diverse series of 1,2,4-oxadiazoles based substituted compounds were designed, synthesized and evaluated as anticancer agents targeting carbonic anhydrase IX (CAIX). Initial structure-activity analysis suggested that the thiazole/thiophene-sulfonamide conjugates of 1,2,4-oxadiazoles exhibited potent anticancer activities with low muM potencies. Compound OX12 exhibited antiproliferative activity (IC50 = 11.1 muM) along with appreciable inhibition potential for tumor-associated CAIX (IC50 = 4.23 muM) isoform. Therefore, OX12 was structurally optimized and its SAR oriented derivatives (OX17-27) were synthesized and evaluated. This iteration resulted in compound OX27 with an almost two-fold increase in antiproliferative effect (IC50 = 6.0 muM) comparable to the clinical drug doxorubicin and significantly higher potency against CAIX (IC50 = 0.74 muM). Additionally, OX27 treatment decreases the expression of CAIX, induces apoptosis and ROS production, inhibited colony formation and migration of colon cancer cells. Our studies provide preclinical rational for the further optimization of identified OX27 as a suitable lead for the possible treatment of CRC.

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

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Iridium-catalyzed borylation of secondary C-H bonds in cyclic ethers

The borylation of secondary C-H bonds, specifically secondary C-H bonds of cyclic ethers, with a catalyst generated from tetramethylphenanthroline and an iridium precursor is reported. This borylation occurs with unique selectivity for the C-H bonds located beta to the oxygen atoms over the weaker C-H bonds located alpha to oxygen atoms. Mechanistic studies imply that the C-H bond cleavage occurs directly at the beta position rather than at the alpha position followed by isomerization of a reaction intermediate.

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

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[…] derivative compound and use thereof (by machine translation)

Pulmonary hypertension or pulmonary arterial pulmonary hypertension [to] (PH) (PAH) used for treating compound. [Solution] the following compounds, or its enantiomers, diastereomers, or a pharmaceutically acceptable salt. In the formula, R20 – R36 Is independently H or deuterium, Z is, alkoxy carbonyl alkoxy group, such as alkoxy carbonyl alkyl amino group represents. [Drawing] no (by machine translation)

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