Category: 14678-05-8

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬Which mentioned a new discovery about 14678-05-8, molcular formula is C3H4N2O, introducing its new discovery. , 14678-05-8

DIHYDROBENZOXAZINE AND TETRAHYDROQUINOXALINE SODIUM CHANNEL INHIBITORS

The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, 14678-05-8, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 14678-05-8

Reference£º
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

14678-05-8, In an article, published in an article,authors is Brown, Dearg S., once mentioned the application of 14678-05-8, Name is Isoxazol-5-amine,molecular formula is C3H4N2O, is a conventional compound. this article was the specific content is as follows.

The discovery of N-cyclopropyl-4-methyl-3-[6-(4-methylpiperazin-1-yl)-4- oxoquinazolin-3(4H)-yl]benzamide (AZD6703), a clinical p38alpha MAP kinase inhibitor for the treatment of inflammatory diseases

A novel, potent and selective quinazolinone series of inhibitors of p38alpha MAP kinase has been identified. Modifications designed to address the issues of poor aqueous solubility and high plasma protein binding as well as embedded aniline functionalities resulted in the identification of a clinical candidate N-cyclopropyl-4-methyl-3-[6-(4-methylpiperazin-1-yl)-4-oxoquinazolin- 3(4H)-yl]benzamide (AZD6703). Optimisation was guided by understanding of the binding modes from X-ray crystallographic studies which showed a switch from DFG ‘out’ to DFG ‘in’ as the inhibitor size was reduced to improve overall properties.

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Reference£º
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

14678-05-8, Isoxazol-5-amine is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred slurry of 4-methyl-3-[6-(4-methylpiperazin-l-yl)-4-oxoquinazolin- 3(4H)-yl]benzoic acid (0.3 g) and DMF (0.05 ml) in methylene chloride (30 ml) at 350C was added thionyl chloride (0.3 ml). The resultant yellow solution was stirred at 45C for 1.5 hours. The reaction mixture was concentrated to give a yellow / orange solid. The solid was stirred in methylene chloride (30 ml) at room temperature with 5-aminoisoxazole (0.11 g) and pyridine (0.2 ml) for 18 hours. The reaction mixture was washed with saturated NaHCO3 solution, brine and concentrated. The residue was purified by column chromatography on a silica column using initially methylene chloride and then a 9:1 mixture of methylene chloride and methanol as eluent. There was thus obtained the title compound (70 mg); NMR Spectrum: (DMSOd6) 2.19 (s, 3H), 2.25 (s, 3H), 2.49 (m, 4H), 3.30 (m, 4H), 6.43 (d, IH), 7.50 (d, IH), 7.62 (s, IH), 7.65 (m, 2H)3 8.08 (s, IH), 8.10 (m, IH), 8.13 (s, IH), 8.50 (d, IH), 12.04 (s, IH); Mass Spectrum: MH-H+ 444., 14678-05-8

The synthetic route of 14678-05-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2006/90143; (2006); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

14678-05-8, Isoxazol-5-amine is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(4) 2,2,2-Trichloroethyl isoxazol-5-ylcarbamate; To a solution of isoxazole-5-amine (740 mg, 8.80 mmol) and pyridine (2.14 ml, 26.4 mmol) in tetrahydrofuran (10 ml) was added 2,2,2-trichloroethyl chloroformate (1.82 ml, 13.2 mmol) with ice-cooling and the mixture was stirred for 40 minutes with ice-cooling. To the mixture was further added 2,2,2-trichloroethyl chloroformate (1.82 ml, 13.2 mmol) with ice-cooling and the mixture was stirred for 30 minutes with ice-cooling, the reaction mixture was poured into ice-water and the mixture was extracted with ethyl acetate. The extract was washed with water and dried over anhydrous magnesium sulfate and the solvent was distilled off under reduced pressure. The residue was purified by silica gel column chromatography (hexane : ethyl acetate = 1 : 1) to obtain the desired product (1.23 g, 53.9%) as a solid. 1H-NMR (CDCl3) delta; 4.87 (2H, s), 6.20 (1H, d, J = 2.1 Hz), 8.00 (1H, br s), 8.18 (1H, d, J = 2.1 Hz).

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Reference£º
Patent; Takeda Pharmaceutical Company Limited; EP1813606; (2007); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.14678-05-8,Isoxazol-5-amine,as a common compound, the synthetic route is as follows.

Example 26-Methyl-4-(3-methyl-lH-indazol-5-yl)-4,7-dihydroisoxazolo[5,4-b]pyridine-5-carbonitrileA mixture of 50 mg (0.22 mmol) (2?)-2-[(3-methyl-lH-indazol-5-yl)methylidene]-3-oxobutane- nitrile (Example 2A) and 19 mg (0.22 mmol) 1 ,2-oxazol-5-amine in propan-2-ol (1.0 ml) was stirred at reflux temperature overnight. The reaction mixture was then concentrated under reduced pressure, and the residue was purified by preparative RP-EtaPLC (acetonitrile/water + 0.1% TFA gradient) to yield 45 mg (69% of th.) of the racemic title compound.LC-MS (method 2): R, = 0.85 min; MS (ESIpos): m/z = 292 (M+Eta)+ 1H-NMR (400 MHz, DMSOd6): delta = 12.63 (br. s, IH), 10.91 (s, IH), 8.14 (s, IH), 7.55 (s, IH), 7.43 (d, IH), 7.19 (d, IH), 5.02 (s, IH), 2.48 (s, 3H), 2.16 (s, 3H) ppm., 14678-05-8

The synthetic route of 14678-05-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BAYER SCHERING PHARMA AKTIENGESELLSCHAFT; MICHELS, Martin; FOLLMANN, Markus; VAKALOPOULOS, Alexandros; ZIMMERMANN, Katja; TEUSCH, Nicole; LOBELL, Mario; WO2011/3604; (2011); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem