Extracurricular laboratory:new discovery of (Tetrahydrofuran-3-yl)methanamine

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Nitroisourea derivative

A novel nitroisourea derivative and a process for producing the same, which is an important intermediate for the production of a nitroguanidine derivative having an insecticidal activity, and a process for producing a nitroguanidine derivative having an insecticidal activity using the nitroisourea derivative. The process for producing a nitroguanidine derivative represented by formula (1), effective as an insecticide is shown by reaction scheme (2): STR1 wherein R1 represents an alkyl group having from 1 to 4 carbon atoms or a benzyl group; R2 represents an alkyl group having from 1 to 4 carbon atoms; R3, R4, R5 and R6 each independently represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms; and Q represents a 5-membered or 6-membered heterocyclic ring having at least one of the following: a nitrogen atom, an oxygen atom or a sulfur atom, one of the hydrogen atoms being substitutable with a halogen atom.

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Extended knowledge of 165253-31-6

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Chemistry is traditionally divided into organic and inorganic chemistry. Formula: C5H11NO, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 165253-31-6

PEST CONTROL COMPOSITION, AND METHOD FOR CONTROLLING PEST

PROBLEM TO BE SOLVED: To provide a pest control composition which exhibits excellent control effectiveness against pests, and to provide a method for controlling pests by using the pest control composition. SOLUTION: The pest control composition contains: a substituted 5-membered heterocyclic carboxylic acid N-containing oxygen (sulfur) 3- to 7-membered saturated heterocyclic ring-substituted alkyl amide exemplified by formula (1), formula (15) or the like; and one or more compounds selected from the following groups I to V. The group I comprises sterilizing agents such as epoxy conazole, the group II comprises insecticides such as imidacloprid, the group III comprises acaricides such as cyfluthrin, the group IV comprises phytotoxicity reducing agents, and the group V comprises plant growth regulators such as gibberellin A3. The method for controlling pests by using the pest control composition is also provided. COPYRIGHT: (C)2015,JPO&INPIT

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Tetrahydrofuran – Wikipedia,
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ORGANIC COMPOUNDS

Disclosed are delta-amino-gamma-hydroxy-omega-aryl-alkanoic acid amide compounds of formula (I)and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.

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Identification of Human Toll-like Receptor 2-Agonistic Activity in Dihydropyridine-Quinolone Carboxamides

Using a multiplexed, reporter gene-based, high-throughput screen, we identified 9-fluoro-7-hydroxy-3-methyl-5-oxo-N-(pyridin-3-ylmethyl)-2,3-dihydro-1H,5H-pyrido[3,2,1-ij]quinoline-6-carboxamide as a TLR2 agonist. Preliminary structure-activity relationship studies on the carboxamide moiety led to the identification of analogues that induce chemokines and cytokines in a TLR2-dependent manner. These results represent new leads for the development of vaccine adjuvants.

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3 – Amino methyl tetrahydrofuran synthetic method (by machine translation)

The invention discloses a 3 – amino methyl tetrahydrofuran synthetic method. The method in order to maleic acid diester as the starting material, by Michael addition, metal borohydride reduction, dehydration cyclization and catalytic hydrogenation reduction of four-step reaction for the synthesis of 3 – amino methyl tetrahydrofuran. The invention synthetic method of mild reaction conditions, high product yield, less pollution emission, simple process operation, is suitable for industrial production. (by machine translation)

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BENZIMIDAZOLE DERIVATIVES AS BROMODOMAIN INHIBITORS

Compounds of formula (I) and salts thereof: wherein R1, R2, R3, R4 are defined herein. Compounds of formula (I) and salts thereof have been found to inhibit the binding of the BET family of bromodomain proteins to, for example, acetylated lysine residues and thus may have use in therapy, for example in the treatment of autoimmune and inflammatory diseases, such as rheumatoid arthritis; and cancers.

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Tetrahydrofuran – Wikipedia,
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FUSED THIAZOLOPYRIMIDINE DERIVATIVES AS MNKS INHIBITORS

The present invention relates to compounds of formulae I and H, or pharmaceutically acceptable salts or esters thereof. Further aspects of the invention relate to pharmaceutical compositions and therapeutic uses of said compounds in the treatment of diseases of uncontrolled cell growth, proliferation and/or survival, inappropriate cellular immune responses, inappropriate cellular inflammatory responses, or neurodegenerative disorders, preferably tauopathies, even more preferably, Alzheimer’s disease.

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Tetrahydrofuran – Wikipedia,
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The invention relates to a benzofuran as raw materials for the synthesis of 3 – amino methyl tetrahydrofuran (by machine translation)

The invention relates to a benzofuran as raw materials for the synthesis of 3 – amino methyl tetrahydrofuran, relates to the technical field of the synthesis intermediate for agricultural chemicals, to benzofuran as raw materials, obtained by the oxidation of the open loop 1, 4 – butene dialdehyde, and nitromethane by Michael addition, sodium borohydride reduction, dehydration cyclization and catalytic hydrogenation to five-step reaction to obtain 3 – amino methyl tetrahydrofuran. The present invention provides a benzofuran as raw materials for the synthesis of 3 – amino methyl tetrahydrofuran, the method cheap price of raw materials, synthetic route is short, low production cost, is suitable for mass production. (by machine translation)

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Analyzing the synthesis route of 165253-31-6

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165253-31-6, (Tetrahydrofuran-3-yl)methanamine is a Tetrahydrofurans compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

EXAMPLE 90 6-methyl-N-(tetrahydro-3-furanylmethyl)nicotinamide A suspension of 6-methylnicotinic acid (6 mmol) in dry dichloromethane (9 mL) was treated with thionyl chloride (12.4 mmol) at 0 C., stirred for one hour, and concentrated in vacuo. The concentrate was added dropwise to a cold solution of (2RS)-tetrahydro-2-furanylmethylamine (6 mmol) and triethylamine (4.5 mL) in dichloromethane (20 mL). The mixture was stirred for 4 hours and then concentrated in vacuo. The residue was dissolved in dichloromethane, washed sequentially with saturated sodium bicarbonate, water, and brine, dried (MgSO4), filtered, and concentrated in vacuo. The crude product was purified by HPLC on a C-18 column using a solvent system increasing in gradient from 5% to 100% acetonitrile/water containing 0.01% TFA over 50 minutes to provide the desired product as the trifluoroacetate salt. MS m/e 221.1 (M+H)+; 1H NMR (DMSO-d6) delta 1.56-1.65 (m, 1H), 1.91-2.00 (m, 1H), 2.44-2.53 (m, 1H), 2.60 (s, 3H), 3.21-3.33 (m, 2H), 3.48 (q, 1H), 3.59-3.65 (m, 1H), 3.69 (q, 1H), 3.72-3.78 (m, 1H), 7.57 (d, 1H), 8.31 (dd, 1H), 8.79 (t, 1H), 8.96 (d, 11H).

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Reference£º
Patent; Haviv, Fortuna; Bradley, Michael F.; Dinges, Jurgen; Sauer, Daryl R.; Henkin, Jack; US2004/67985; (2004); A1;,
Tetrahydrofuran – Wikipedia
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Downstream synthetic route of 165253-31-6

165253-31-6 (Tetrahydrofuran-3-yl)methanamine 10898660, aTetrahydrofurans compound, is more and more widely used in various.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.165253-31-6,(Tetrahydrofuran-3-yl)methanamine,as a common compound, the synthetic route is as follows.

A 0.5-2 mL microwave vial containing a stir bar was placed under argon by attaching a rubber septum and performing 4 vacuum/argon cycles. The intermediate from Example 9 Step C (100 mg, 0.146 mmol), sodium tert-butoxide (20.99 mg, 0.218 mmol), 2-(di- tert-butylphosphino)biphenyl (8.7 mg, 0.029 mmol), Pd2(dba)3 (13.33 mg, 0.015 mmol) were added, and the vial was sealed. While adding the solids to the vial, 30 mL of toluene was deoxygenated by bubbling argon through for 30 minutes; 1.0 mL of this was added to the sealed reaction vial. 3-(Aminomethyl)tetrahydrofuran (0.024 ml, 0.204 mmol) was added via microsyringe, and men argon was flushed gently through the vial for 5 min. The reaction was heated to 90C for 15 hours and then cooled to room temperature. A solution of tetrabutylammonium fluoride (1 M in tetrahydrofuran, 0.710 ml, 0.710 mmol) was added, and the vial was heated in a microwave oven for 10 min at 1500C. After cooling to room, temperature, the reaction mixture was partitioned between a 1 :1 mixture of EtOAc: ether (20 mL) and water (10 mL). The layers were separated, and the organic layer was washed sequentially with water (10 mL), saturated NaHCtheta3 (10 mL), and brine (10 mL), dried over Na2SO4, filtered, and concentrated. The resulting solid was purified by reverse phase HPLC. After lypophilization, the title compound was obtained. 1H NMR (600 MHz, DMSO) delta: 11.44 (s, 1 H), 9.57 (s, 1 H), 8.22 (m, 1 H), 7.68 (m, 1 H), 7.49 (t, 1 H, J= 6.3 Hz), 7.38 (t, 2 H, J= 8.2 Hz), 7.16 (d, 2 H, J= 5.6 Hz), 3.78 (m, 2 H), 3.64 (q, 1 H, J= 7.6 Hz), 3.51 (dd, 1 H, J= 8.5, 5.6 Hz), 3.17 (m, 2 H), 2.60 (m, 1 H), 2.04 (m, 1 H), 1.66 (m, 1 H): [M+l]+ 447.

165253-31-6 (Tetrahydrofuran-3-yl)methanamine 10898660, aTetrahydrofurans compound, is more and more widely used in various.

Reference£º
Patent; MERCK & CO., INC.; WO2007/145957; (2007); A1;,
Tetrahydrofuran – Wikipedia
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