Some scientific research about (R)-Tetrahydrofuran-3-amine 4-methylbenzenesulfonate

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Synthetic Route of 111769-27-8, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.111769-27-8, Name is (R)-Tetrahydrofuran-3-amine 4-methylbenzenesulfonate, molecular formula is C11H17NO4S. In a Article£¬once mentioned of 111769-27-8

5′-C-ethyl-tetrazolyl-N 6-substituted adenosine and 2-chloro-adenosine derivatives as highly potent dual acting A1 adenosine receptor agonists and A3 adenosine receptor antagonists

A series of N6-substituted-5′-C-(2-ethyl-2H-tetrazol-5-yl)-adenosine and 2-chloro-adenosine derivatives was synthesized as novel, highly potent dual acting hA1AR agonists and hA3AR antagonists, potentially useful in the treatment of glaucoma and other diseases. The best affinity and selectivity profiles were achieved by N6-substitution with a 2-fluoro-4-chloro-phenyl-or a methyl-group. Through an in silico receptor-driven approach, the molecular bases of the hA1-and hA3AR recognition and activation of this series of 5′-C-ethyl-tetrazolyl derivatives were explained.

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

Final Thoughts on Chemistry for (R)-Tetrahydrofuran-3-amine 4-methylbenzenesulfonate

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Electric Literature of 111769-27-8, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.111769-27-8, Name is (R)-Tetrahydrofuran-3-amine 4-methylbenzenesulfonate, molecular formula is C11H17NO4S. In a Patent£¬once mentioned of 111769-27-8

NEW PYRIDINE DERIVATIVES AS LEPTIN RECEPTOR MODULATOR MIMETICS

The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.

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

Properties and Exciting Facts About (R)-Tetrahydrofuran-3-amine 4-methylbenzenesulfonate

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Free-wilson and structural approaches to Co-optimizing human and rodent isoform potency for 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitors

11beta-Hydroxysteroid dehydrogenase 1 (11beta-HSD1) has been a target of intensive research efforts across the pharmaceutical industry, due to its potential for the treatment of type II diabetes and other elements of the metabolic syndrome. To demonstrate the value of 11beta-HSD1 in preclinical models, we required inhibitors with good potency against both human and rodent isoforms. Herein, we describe our efforts to understand how to co-optimize human and murine potency within the (5-hydroxy-2-adamantyl)-pyrimidine-5-carboxamide series. Two approaches are described-a data-driven (Free-Wilson) analysis and a structure-based design approach. The conclusions from these approaches were used to inform an efficient campaign to design compounds with consistently good human/murine potency within a logD7.4 range of 1-3. Compounds 20 and 26 demonstrated good rodent PK, which allowed us to demonstrate a PK/PD relationship in rat and mouse. We then evaluated 26 against glycemic and body weight end points in murine disease models, where it demonstrated glucose and body weight efficacy at 300 mg/kg/day but only body weight efficacy at 50 mg/kg/day, despite providing >90% target engagement in the liver.

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

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Adamantyl Iminocarbonyl-Substituted Pyrimidines As Inhibitors Of 11-Beta-HSD1 826

A compound of formula (I): and pharmaceutically-acceptable salts thereof, wherein the variable groups are defined within; their use in the inhibition of 112HSD1, processes for making them and pharmaceutical compositions comprising them are also described herein.

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

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PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS

The invention relates to a compound of formula (I) or a salt thereof: wherein:R1 is C1-4alkyl, C1-3fluoroalkyl, -CH2CH2OH or -CH2CH2CO2C1-2alkyl;R2 is a hydrogen atom (H), methyl or C1fluoroalkyl;R3 is optionally substituted C3-8cycloalkyl or optionally substituted mono-unsaturated-C5-7cycloalkenyl or an optionally substituted heterocyclic group of sub-formula (aa), (bb) or (cc); in which n1 and n2 independently are 1 or 2; and in which Y is O, S, SO2, or NR10; or R3 is a bicyclic group (dd) or (ee):; and wherein X is NR4R5 or OR5a. The compounds are phosphodiesterase (PDE) inhibitors, in particular PDE4 inhibitors. Also provided is the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment and/or prophylaxis of an inflammatory and/or allergic disease in a mammal such as a human, for example chronic obstructive pulmonary disease (COPD), asthma, or allergic rhinitis.

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Tetrahydrofuran – Wikipedia,
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SUBSTITUTED 2-PHENYL-PYRIDINE DERIVATIVES

The present invention relates to compounds of formula I wherein R1, R2, R4, R5, Ra, Rb, n, W and Z are as defined in the application, their preparation and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.

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

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TRIAZOLOPYRIDINE COMPOUNDS

The invention is concerned with triazolopyridine compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as pharmaceuticals.

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

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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.111769-27-8,(R)-Tetrahydrofuran-3-amine 4-methylbenzenesulfonate,as a common compound, the synthetic route is as follows.

To a solution of (2,6-dimethylpyridin-4-yl)methyl 4-nitrophenyl carbonate (Intermediate 2;235 mg, 0.78 mmol) in DMF (5 mL) was added DIPEA (400 muL, 2.3 mmol), (R)- tetrahydrofuran-3 -amine toluenesulfonate (221 mg, 0.85 mmol) and DMAP (10 mg, catalytic). The reaction mixture was stirred overnight and then concentrated in vacuo. The residue was dissolved in EtOAc (25 mL), washed with IM aq Na2CO3 solution (5 x 25 mL), dried (MgSO4) and concentrated in vacuo. The residue was dissolved in DCM (5 mL) and treated with 2M HCl in Et2O (0.5 mL, 1.0 mmol) to give a precipitate. The – -solvent was removed by decantation and the precipitate was dried in vacuo to give (2,6- dimethylpyridin-4-yl)methyl (3R)-tetrahydrofuran-3-ylcarbamate hydrochloride (102 mg, 46%) as a white solid.Analytical HPLC: purity 99.3% (System A, Rtau = 3.03 min); Analytical LCMS: purity 100% (System E, Rtau = 4.59 min), ES+: 251.4 [MH]+; HRMS calcd for Ci3Hi8N2O3: 250.1317, found 250.1330.

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Reference£º
Patent; BIOVITRUM AB (PUBL); WO2009/147216; (2009); A1;,
Tetrahydrofuran – Wikipedia
Tetrahydrofuran | (CH2)3CH2O – PubChem

Downstream synthetic route of 111769-27-8

111769-27-8 (R)-Tetrahydrofuran-3-amine 4-methylbenzenesulfonate 14243169, aTetrahydrofurans compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.111769-27-8,(R)-Tetrahydrofuran-3-amine 4-methylbenzenesulfonate,as a common compound, the synthetic route is as follows.

Example 294-((R)-2-{[6-phenyl-(R)-4-(tetrahydro-furan-3-ylamino)-pyridine-2-carbonyl]-amino}-3-phosphono-propionyl)-piperazine-1-carboxylic acid butyl ester29.1. 4-{3-(ethoxy-hydroxy-phosphoryl)-2-[(6-phenyl-4-pyrrolidin-1-yl-pyridine-2-carbonyl)-amino]-propionyl}-piperazine-1-carboxylic acid butyl esterA reaction mixture containing intermediate 25.1 (100 mg), (R)-(+)-3-aminotetrahydrofurane to luene-4-sulfonate (43 mg), acetato (2′-di-tert-butylphosphino-1,1′-biphenyl-2-yl)palladium (9.7 mg) and NaOtBu (46 mg) in toluene (1 mL) at 90 C. under argon until reaction completion. The solvent was evaporated in vacuo and the crude product (119 mg) used without further purification.LC-MS: tR=0.78 min; [M+H]+: 632.16., 111769-27-8

111769-27-8 (R)-Tetrahydrofuran-3-amine 4-methylbenzenesulfonate 14243169, aTetrahydrofurans compound, is more and more widely used in various fields.

Reference£º
Patent; Caroff, Eva; Hilpert, Kurt; Hubler, Francis; Meyer, Emmanuel; Renneberg, Dorte; US2011/46089; (2011); A1;,
Tetrahydrofuran – Wikipedia
Tetrahydrofuran | (CH2)3CH2O – PubChem

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111769-27-8, (R)-Tetrahydrofuran-3-amine 4-methylbenzenesulfonate is a Tetrahydrofurans compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

l-(5,6-Dichloro-lH-benzo[d]imidazol-2-yl)piperidine-4-carboxylic acid (628 mg, 2.0 mmol), (R)-(+)-tetrahydrofuran-3 -amine 4-methylbenzenesulfonate (622 mg, 2.4 mmol), 2-(7-aza-lH- benzotriazole-l-yl)-l, l,3,3-tetramethyluronium hexafluorophosphate (HATU, 912 mg, 2.4 mmol), N,N-diisopropylethylamine (Hiinig’s base, DIEA, 775 mg, 6.0 mmol) and N,N- dimethylformamide (25 mL) was stirred at room temperature for 100 minutes. The reaction mixure was concentrated in vacuo, the residue purified on column (silica gel, flashchromatography, dichloromethane/methanol, gradient elution 4-20 % methanol) and finally precipitated from chloroform to give 378 mg (49 % yield) of (R)-l-(5,6-dichloro-lH- benzo[d]imidazol-2-yl)-N-(tetrahydrofuran-3-yl)piperidine-4-carboxamide as a white solid. LC- MS (m/z) 382.9 (M+l)., 111769-27-8

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Reference£º
Patent; NOVASAID AB; WANNBERG, Johan; ALTERMAN, Mathias; MALM, Johan; WO2012/117062; (2012); A1;,
Tetrahydrofuran – Wikipedia
Tetrahydrofuran | (CH2)3CH2O – PubChem