Tag: 1136-45-4

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1136-45-4,5-Methyl-3-phenylisoxazole-4-carboxylic acid,as a common compound, the synthetic route is as follows.

A solution of 5-methyl-3-phenylisoxazole-4-carboxylic acid (60 mg, 0.3 mmol), DIEA (46 mg, 0.36 mmol), and DPPA (100 mg, 0.38 mmol) in toluene (1 mL) was shaken for 30 minutes at room temperature and then heated and shaken at 90 C for 16 h. The reaction mixture was then added to the resin from step A and mixture shaken for 5 h at 90 C. The reaction mixture was filtered and the resin was washed with 3 times each with DMF, 1 : 1 acetic acid/DCM, water, isopropanol and finally with DCM. The resin was then dried in a vacuum oven for 2 h., 1136-45-4

1136-45-4 5-Methyl-3-phenylisoxazole-4-carboxylic acid 14343, aIsoxazoles compound, is more and more widely used in various.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; COOKE, Andrew, J.; STUMP, Craig, A.; ZHANG, Xu-Fang; LI, Chun Sing; MAO, Qinghua; WO2015/42085; (2015); A2;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

1136-45-4, 5-Methyl-3-phenylisoxazole-4-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5-Methyl-3-phenylisooxazole-4-carboxylic acid (40 mg, 0.197 mmol), 1-(2-(1-Pyrrolidinyl)-ethyl)-piperazine (39.4 mg, 0.215 mmol), O-(benzotriazol-1-yl)-N,N,N’,N’-tetramethyluronium tetrafluoroborate (86.2 mg, 0.268 mmol) and diisopropylethylamine (25.4 mg, 0.197 mmol) were mixed in dimethylformamide (1.5 mL) and stirred at room temperature. Solvent was evaporated in vacuo, and the residue was taken up in methanol (1 mL), filtered and purified by preparative chromatography. The combined fractions were partitioned between NaHCO3 (sat) and ethylacetate. The organic layer was washed with water and concentrated in vacuo to afford the title compound. HRMS (ESI, pos. ion) m/z calcd for C21H28N4O2: 368.2212, found 368.2217.

1136-45-4, 1136-45-4 5-Methyl-3-phenylisoxazole-4-carboxylic acid 14343, aIsoxazoles compound, is more and more widely used in various.

Reference£º
Patent; Amgen Inc.; Biovitrum AB; US2008/21022; (2008); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

1136-45-4, 5-Methyl-3-phenylisoxazole-4-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 5-methyl-3-phenylisoxazole-4-carboxylic acid (8.00 g, 39.4 mmol) and DMF (200 mL) was cooled to 0-10 C. N,N-Diethyl-p-phenylenediamine (6.47 g, 39.4 mmol) and O-ibenzotriazol- l-yl)-N,N,N’,N’ -tetramethyluronium tetrafluoroborate (TBTU, 15.17 g, 47.3 mmol, 1.2 equiv.) were added to the reaction mixture and the mixture was stirred at 0-10 C for 10 min. Nu,Nu-Diisopropylethylamine (DIPEA, 6.11 g, 47.3 mmol, 1.2 equiv.) was slowly added, and the mixture was stirred at 0-10C for 2.5 h. Ethyl acetate (400 mL) and a 5% aqueous NaHC03-solution (160 mL) were added to the reaction mixture and the mixture was stirred at ambient temperature for 15 min. The layers were separated and the organic phase was washed with water (3 x 200 mL) and brine (180 mL). The organic layer was dried with sodium sulphate, the drying agent was filtered off and the solution was evaporated to dryness to give 12.8 g of the crude product. The crude product was dissolved in warm ethyl acetate (300 mL) and activated carbon (0.5 g) was added to the solution. The mixture was stirred for 20 min and filtered through Celite. n-Heptane (120 mL) was added to the previous solution at 55 C and the mixture slowly cooled to 0-5 C. The precipitated product was filtered off, washed with n-heptane (2 x 50 mL) and dried in vacuo at 45 C overnight to give 8.52 g (62 %) off-white powder. M.p. 139.3-140.2 C. 1H NMR (200 MHz, DMSO-d6) delta 10.12 (s, 1H, NH), 7.71 (m, 2H, arom), 7.50-7.35 (m, 5H arom.), 6.63 (d, 2H, arom.), 3.30 (q, 4H, 2 x CH2), 2.55 (s, 3H, CH3), 1.05 (t, 6H, 2 x CH3) ppm. MS: m/z 350.2 (100%, M+l), 351.2 (25%).

The synthetic route of 1136-45-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; UNIVERSITY OF HELSINKI; UNIVERSITY OF OULU; KINNUNEN, Sini; TOeLLI, Marja; VAeLIMAeKI, Mika; JUMPPANEN, Mikael; BOIJE AF GENNAeS, Gustav; YLI-KAUHALUOMA, Jari; RUSKOAHO, Heikki; (75 pag.)WO2018/55235; (2018); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

1136-45-4, 5-Methyl-3-phenylisoxazole-4-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A solution of 5-methyl-3-phenylisoxazole-4-carboxylic acid (1.01 g, 4.97 mmol) and DMF (25 mL) was cooled to 0-10 C. N-(4-Chlorophenyl)-4-methyl-4,5-dihydrothiazol-2-amine (1.12 g, 4.94 mmol) and O-ibenzotriazol- l-y^-N.N.N’.N’-tetramethyluronium tetrafluoroborate (TBTU, 1.90 g, 5.92 mmol) were added to the reaction mixture and the mixture stirred at 0-10 C for 10 min. DIPEA (0.78 g, 6.04 mmol) was slowly added to the reaction mixture and the mixture stirred at 0-10 C for 4 h. The cooling bath was removed and the mixture was stirred for further 50 min allowing it to warm up to rt. EtOAc (40 mL) and an 10% aqueous NaHC03- solution (35 mL) were added to the reaction mixture and the mixture was stirred at rt for 5 min. The layers were separated and the organic layer was washed with water (3 x 30 mL) and brine (15 mL). The organic layer was dried with Na2S04, the drying agent was filtered off and the solvents were evaporated in vacuo to give the crude product. It was dissolved in EtOAc (10- 12 mL) at rt and the solution was stirred for 15 min, during the time the product started to crystallize out of the solution. n-Heptane (20 mL) was added and the mixture was stirred at rt for 15 min, during the time more product precipitated. The precipitated product was filtered off, it was washed with n- heptane and dried in vacuo at 50 C overnight to give the product as a white powder (1.53, 75%). 1H NMR (200 MHz, CDC13): delta .6-1 A (m, 5H, arom.), 7.2-7.1 (m, 2H, arom.), 6.4- 6.3 (m, 2H arom.), 4.6-3.5 (broad m, 2H, thiazole CH2), 3.5 (m, 1H, thiazole CH), 2.6 (s, 3H, Me), 1.4 (d, 3H, thiazole Me) ppm.

1136-45-4 5-Methyl-3-phenylisoxazole-4-carboxylic acid 14343, aIsoxazoles compound, is more and more widely used in various.

Reference£º
Patent; UNIVERSITY OF HELSINKI; UNIVERSITY OF OULU; KINNUNEN, Sini; TOeLLI, Marja; VAeLIMAeKI, Mika; JUMPPANEN, Mikael; BOIJE AF GENNAeS, Gustav; YLI-KAUHALUOMA, Jari; RUSKOAHO, Heikki; (75 pag.)WO2018/55235; (2018); 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.1136-45-4,5-Methyl-3-phenylisoxazole-4-carboxylic acid,as a common compound, the synthetic route is as follows.

To a solution of 5-methyl-3-phenyl-isoxazole-4-carboxylic acid (5.00 g, 24.6 mmol) in THF (50 mL) was added in one portion l,l’-carbonyl-diimidazole (4.39 g, 27.1 mmol). After stirring for 15 min at ambient temperature the solution was warmed to 70 0C and stirred for 30 min at this temperature. After the solution was cooled to 0 0C hydrazine monohydrate (2.4 mL, 49.0 mmol) was added over a period of 2 min while the temperature raised to 15 0C. The resulting suspension was stirred for 30 min at 0 0C. After addition of 20 mL heptane the suspension was stirred for 15 min at 0 0C and filtered off. Washing with water and drying afforded the title compound (4.52 g, 85%) as a white solid. MS: m/e = 218.2 [M+H]+.

The synthetic route of 1136-45-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; WO2007/71598; (2007); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

1136-45-4, 5-Methyl-3-phenylisoxazole-4-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5-Methyl-3-phenylisooxazole-4-carboxylic acid (40 mg, 0.197 mmol), 3-(teroom temperature-Butoxycarbonylamino)pyrrolidine (40 mg, 0.215 mmol), O-(benzotriazol-1-yl)-N,N,N’,N’-tetramethyluronium tetrafluoroborate (86.2 mg, 0.268 mmol) and diisopropylethylamine (25.4 mg, 0.197 mmol) were mixed in dimethylformamide (1.5 mL) and stirred at room temperature. Solvent was evaporated in vacuo, and the residue was taken up in methanol (1 mL), filtered and purified by preparative chromatography. The combined fractions were partitioned between NaHCO3 (sat) and ethylacetate. The organic layer was washed with water and concentrated in vacuo to afford the title compound. HRMS (ESI, pos. ion) m/z calcd for C20H25N3O4: 371.1845, found 371.1851.

As the paragraph descriping shows that 1136-45-4 is playing an increasingly important role.

Reference£º
Patent; Amgen Inc.; Biovitrum AB; US2008/21022; (2008); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

1136-45-4, 5-Methyl-3-phenylisoxazole-4-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 1 g (10 mmol) but-2-ynoyl chloride (Journal of Organic Chemistry (1981), 46(11), 2273-80), 0.625 g (5 mmol) 5-Methyl-3-phenyl-isoxazole-4-carboxylic acid (commercially available) and 1.3 g (10 mmol) AlCl3 in 10 mL dichloroethane was at room temperature for 18 h. The mixture was poured onto ice/water and the organic layer washed with Na2CO3 sat., NaCl sat. and dried with Na2SO4. After evaporation of all volatiles the residue was purified on silica eluting with a gradient of ethyl acetate and heptane affording 0.2 g (17%) of the title compound as light brown solid. (m/e): 227.1 (M+).

The synthetic route of 1136-45-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Buettelmann, Bernd; Han, Bo; Knust, Henner; Nettekoven, Matthias Heinrich; Thomas, Andrew William; US2007/66668; (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.1136-45-4,5-Methyl-3-phenylisoxazole-4-carboxylic acid,as a common compound, the synthetic route is as follows.

5-Methyl-3-phenylisooxazole-4-carboxylic acid (40 mg, 0.197 mmol), ethyl isonipecotate (33.8 mg, 0.215 mmol), O-(benzotriazol-1-yl)-N,N,N’,N’-tetramethyluronium tetrafluoroborate (86.2 mg, 0.268 mmol) and diisopropylethylamine (25.4 mg, 0.197 mmol) were mixed in dimethylformamide (1.5 mL) and stirred at room temperature. Solvent was evaporated in vacuo, and the residue was taken up in methanol (1 mL), filtered and purified by preparative chromatography. The combined fractions were partitioned between NaHCO3 (sat) and ethylacetate. The organic layer was washed with water and concentrated in vacuo to afford the title compound. HRMS (ESI, pos. ion) m/z calcd for C19H22N2O4: 342.1580, found 342.1578.

As the paragraph descriping shows that 1136-45-4 is playing an increasingly important role.

Reference£º
Patent; Amgen Inc.; Biovitrum AB; US2008/21022; (2008); 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.1136-45-4,5-Methyl-3-phenylisoxazole-4-carboxylic acid,as a common compound, the synthetic route is as follows.

A mixture of 406 mg (2 mmol) 5-methyl-3-phenyl-isoxazole-4-carboxylic acid (commercially available) and 4 mL SOCl2 was heated to reflux for 3 h. After evaporation of all volatiles the residue was added to a mixture of 206 mg (2 mmol) 1H-pyrrole-2-carboxylic acid methyl ester (commercially available) and 440 mg (3 mmol) AMCl3 in 25 mL dichloroethane and heated to reflux for 3 h. After cooling to room temperature the precipitate was collected and washed with dichloromethane. The residue was purified on silica eluting with a gradient of ethyl acetate and heptane affording 210 mg (37%) of the title compound as white foam. (m/e): 311.0 (MH+; 100%).

1136-45-4 5-Methyl-3-phenylisoxazole-4-carboxylic acid 14343, aIsoxazoles compound, is more and more widely used in various.

Reference£º
Patent; Buettelmann, Bernd; Han, Bo; Knust, Henner; Nettekoven, Matthias Heinrich; Thomas, Andrew William; US2007/66668; (2007); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

1136-45-4, 5-Methyl-3-phenylisoxazole-4-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

5-Methyl-3-phenylisooxazole-4-carboxylic acid (40 mg, 0.197 mmol), 3-(pyrrolidin-2-ylmethyl)pyridine (50.5 mg, 0.215 mmol), O-(benzotriazol-1-yl)-N,N,N’,N’-tetramethyluronium tetrafluoroborate (86.2 mg, 0.268 mmol) and diisopropylethylamine (25.4 mg, 0.197 mmol) were mixed in dimethylformamide (1.0 mL) and stirred at room temperature. Solvent was evaporated in vacuo, and the residue was taken up in methanol (1 mL), filtered and purified by preparative chromatography. The combined fractions were partitioned between NaHCO3 (sat) and ethylacetate. The organic layer was washed with water and concentrated in vacuo to afford the title compound. HRMS (ESI, pos. ion) m/z calcd for C21H21N3O2: 349.1426, found 349.1693.

As the paragraph descriping shows that 1136-45-4 is playing an increasingly important role.

Reference£º
Patent; Amgen Inc.; Biovitrum AB; US2008/21022; (2008); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem