Category: 1018297-63-6

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1018297-63-6,(3-(4-Fluorophenyl)-5-methylisoxazol-4-yl)methanol,as a common compound, the synthetic route is as follows.

4.98 g (24.0 mmol) of [3-(4-fluorophenyl)-5-methyl-1 ,2-oxazol-4-yl]methanol (WO 2013/057123 A1 , Hoffmann-La Roche) was dissolved in 80 ml_ of anhydrous dichloromethane, and 9.76 g (3.39 ml_, 36.1 mmol) of phosphorus tribromide was added dropwise to the stirred solution. The reaction mixture was stirred for 1 hour at room temeprature, and poured into 50 ml_ of saturated sodium bicarbonate solution. The mixture was stirred for another 10 minutes, and the phases were separated. The organic phase was washed with water, dried over anhydrous sodium sulfate, and evaporated to afford 5.89 g (97%) of the title compound as a yellow-brownish solid. MS (ESI) m/z: 269.9 [M+H]+., 1018297-63-6

1018297-63-6 (3-(4-Fluorophenyl)-5-methylisoxazol-4-yl)methanol 28473136, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; RICHTER GEDEON NYRT.; SZABO, Gyoergy; TUROS, Gyoergy Istvan; ELIAS, Oliver; KAROLYI, Benedek Imre; ERDELYI, Peter; KAPUS, Gabor Laszlo; (75 pag.)WO2020/65597; (2020); 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.1018297-63-6,(3-(4-Fluorophenyl)-5-methylisoxazol-4-yl)methanol,as a common compound, the synthetic route is as follows.

Step e: 6- r3-(4-Fluoro-phenyl)-5-methyl-isoxazol-4-ylmethoxyl -nicotinic acid methyl ester: To a suspension of sodium hydride (55% dispersion in mineral oil, 852 mg, 20 mmol) in THF (27 mL) was added a solution of [3-(4-fluoro-phenyl)-5-methyl-isoxazol-4-yl]-methanol (103 mg, 0.55 mmol) (3.68 g, 18 mmol) in THF (54 mL) at 0 C and the reaction mixture warmed to room temperature over 30 min. Then a solution of methyl 6-chloronicotinate (3.35 g, 20 mmol) in THF (1.5 mL) was added dropwise at 0 C and the reaction mixture was stirred at room temperature overnight. The reaction mixture was then poured into aqueous sodium chloride (saturated) and the mixture was extracted with ethyl acetate. The combined organic layers were then washed with water and brine and then dried over sodium sulfate, filtered and evaporated. Purification by chromatography (Si02, heptane:ethyl acetate = 7:3) afforded the title compound (81 mg, 47%) which was obtained as a light yellow solid. MS: m/e = 343.3 [M+H]+., 1018297-63-6

As the paragraph descriping shows that 1018297-63-6 is playing an increasingly important role.

Reference£º
Patent; IP Gesellschaft fuer Management mbH; Trinius, Frank; EP2792360; (2014); 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.1018297-63-6,(3-(4-Fluorophenyl)-5-methylisoxazol-4-yl)methanol,as a common compound, the synthetic route is as follows.

To a solution of [3-(3-fluoro-phenyl)-5-methyl-isoxazol-4-yl]-methanol (5.0 g, 24 mmol) in THF (290 mL) was added phthalimide (4.7 g, 32 mmol) and triphenylphosphine (8.4 g, 32 mmol) at ambient temperature under an argon atmosphere. Then a solution of diethyl azodicarboxylate (40% in toluene, 12.5 mL, 32 mmol) was added and the reaction mixture was stirred for 1 h at room temperature. Concentration and repeated trituration and then purification by chromatography (SiO2, heptane:ethyl acetate=100:0 to 1:1) afforded the title compound (6.0 g, 74%) as a white solid. MS: m/e=337.1 [M+H]+.

1018297-63-6, 1018297-63-6 (3-(4-Fluorophenyl)-5-methylisoxazol-4-yl)methanol 28473136, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; Buettelmann, Bernd; Jakob-Roetne, Roland; Knust, Henner; Lucas, Matthew C.; Thomas, Andrew; US2009/143371; (2009); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

1018297-63-6, (3-(4-Fluorophenyl)-5-methylisoxazol-4-yl)methanol is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Alternative 2: Telescoped process To as suspension of sodium hydride (60% in mineral oil, 3.95 g, 99 mmol, 1.6 eq.) in THF (120 mL) was added within 120 minutes at 25-32C a solution of [3-(4-Fluorophenyl)-5-methyl- isoxazol-4-yl] -methanol (12.50 g, 60 mmol) and 6-chloronicotinonitrile (8.36 g, 60 mmol) in THF (60 mL) and the resulting mixture was stirred for one hour at approx. 30C. The mixture was then treated drop wise at room temperature with water (100 mL). THF was distilled off under reduced pressure (200-70 mbar) with a jacket temperature of 50C. The residue was diluted with ethanol (90 mL) and subsequently treated at 20 to 35C with 28% sodium hydroxide solution (69.6 g, 487 mmol). The mixture was heated to 50-55C and subsequently stirred at this temperature for 15 hour. The reaction mixture was treated with toluene (150 mL) and the resulting biphasic mixture was stirred for 15 minutes and the layers were then allowed to separate for 30 minutes. The lower product-containing aqueous layer was separated and the toluene layer was extracted at 30C with water (1×50 mL). The combined aqueous layers were acidified with 20% sulfuric acid (approx. 150 g) until a pH of 3.0-3.3 was obtained. The suspension was treated with THF (120 mL) and the resulting biphasic mixture was stirred for 15 minutes and the layers were then allowed to separate for 30 minutes. The lower aqueous layer was removed and the product-containing organic layer was diluted with toluene (150 mL) to afford a biphasic mixture from which the lower aqueous layer was separated. The aqueous layer was removed and the organic layer was washed with water (2×30 mL). From the organic layer THF, Ethanol and water were then completely distilled off under reduced pressure and at a jacket temperature of 40-80C and continuously replaced by toluene (250 mL in total). At the end of the distillation a volume of approx. 300 mL was adjusted in the reactor. The partly precipitated product was completely re-dissolved by heating the suspension to 100-105C. The clear solution was cooled to 15-20C within 5-10 hours whereupon crystallization occurred. The crystals were filtered off, washed with toluene (100 mL) and subsequently dried at 55C/

1018297-63-6, As the paragraph descriping shows that 1018297-63-6 is playing an increasingly important role.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; DOTT, Pascal; HANLON, Steven Paul; HILDBRAND, Stefan; IDING, Hans; THOMAS, Andrew; WALDMEIER, Pius; WO2013/57123; (2013); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem