Category: 3405-77-4

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.3405-77-4,5-Methylisoxazole-3-carboxylic acid,as a common compound, the synthetic route is as follows.

Example 1. Compound of formula B, wherein R = (compound 31).To a solution of compound A (25.0 mg, 0.039 mmol), S-methylisoxazole-S-carboxylic acid (5.4 mg, 0.043 mmol) and HATU (16.2 mg, 0.043 mmol) in DMF (0.5 mL) was added diisopropylethylamine (15.0 mg, 0.116 mmol). The reaction mixture was stirred at 25 0C for 16 h and then evaporated under a positive flow of nitrogen. The residue was purified by reverse phase chromatography to give the desired product (20.8 mg, 71percent yield). MS (ESI): m/z = 755.1 [M+H]., 3405-77-4

3405-77-4 5-Methylisoxazole-3-carboxylic acid 76947, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; ENANTA PHARMACEUTICALS, INC.; WO2009/73713; (2009); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

3405-77-4, 5-Methylisoxazole-3-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a 0¡ã C. solution of (054) and 5-methyl-isoxazole-3-carboxylic acid (009) (127 mg, 1.0 mmol), HOBT (135 mg, 1.0 mmol) and HBTU (350 mg, 1.0 mmol) in tetrahydrofuran (100 mL) was added a solution of N,N-diisopropylethylamine (0.5 mL) in tetrahydrofuran (2 mL). The mixture was stirred at room temperature for 5 hours. It was then diluted with ethyl acetate (200 mL) and washed with saturated aqueous sodium bicarbonate (2.x.10 mL) and brine (10 mL). The organic layers were dried over sodium sulfate and filtered through Celite-545, the solvents were removed under reduced pressure and the residue was purified by HPLC (aqueous ammonium acetate and acetonitrile) to provide (055) (40 mg) which was characterized by LC/MS (LCRS (MH) m/z: 576.27); >80percent proteasome CT-L inhibition at 20 mg/kg PO.

3405-77-4, As the paragraph descriping shows that 3405-77-4 is playing an increasingly important role.

Reference£º
Patent; Proteolix, Inc.; US2007/105786; (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.3405-77-4,5-Methylisoxazole-3-carboxylic acid,as a common compound, the synthetic route is as follows.

To a solution of carboxylic acid (5 g) in CH2Cl2 (400 ml) at 0 C. was added N(OCH3)CH3.HCl (11.5 g), DEC (15.1 g), HOBt (5.3 g) and NMM (43 ml) and stirred for 14 hr. The mixture was diluted with CH2Cl2 (100 ml) and the organic layer was washed with 10percent HCl, saturated sodium bicarbonate and brine, dried with Na2SO4, and concentrated in vacuo to afford 5.74 g of crude product (85percent)., 3405-77-4

The synthetic route of 3405-77-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Schering Corporation; US2004/106794; (2004); 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.3405-77-4,5-Methylisoxazole-3-carboxylic acid,as a common compound, the synthetic route is as follows.

Step 5. A solution of 5-methylisoxazole-3-carboxylic acid (8.6 mg, 68 mumol), diisopropylethylamine (12 muL, 68 mumol), and 2-chloro-5-(1-((R)-1-(3-chlorophenyl)ethylamino)ethyl)benzenamine 109 (21 mg, 68 mumol) in DMF was stirred under N2 and chilled to 0¡ã C. HATU (26 mg, 68 mumol) was then added to the solution. The reaction was allowed to warm to room temperature and stirred for 3 h. Afterwards, the reaction was diluted with water and EtOAc. The organic solution was extracted with saturated NaHCO3, water, and brine. The organic layer was dried over MgSO4, filtered, and concentrated in vacuo. The crude material was purified by silica gel chromatography using a 5percent to 60percent gradient of EtOAc in hexanes as the eluent. The desired fractions were combined and concentrated to give N-(2-chloro-5-(1-((R)-1-(3-chlorophenyl)ethylamino)ethyl)phenyl)-5-methylisoxazole-3-carboxamide 110 (20 mg, 70percent yield) as a colorless oil and as a mixture of diastereomers. 1H NMR (400 MHz, MeOH) delta ppm 1.60-1.66 (m, 6H) 2.53 (s, 3H) 4.19 (m, 2H) 6.61 (s, 1H) 7.19 (dd, J=8.31, 2.05 Hz, 1H) 7.30 (m, 1H) 7.40 (s, 1H) 7.48 (d, J=4.89 Hz, 2H) 7.63 (d, J=8.41 Hz, 1H) 8.09 (s, 1H). Mass spectrum: calculated for C21H21Cl2N3O2 418.3; found 418.4 (M++1)., 3405-77-4

The synthetic route of 3405-77-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Amgen Inc.; US2008/221101; (2008); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

3405-77-4, 5-Methylisoxazole-3-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,3405-77-4

(R)-Methyl 3-(5-methyl isoxazole-3-carboxamido)-2,3-dihydro-1H-indene-5-carboxylate (B-25)HATU (4.4 g, 11.7 mmol, 1.5 eq) and DIPEA (3.0 ml, 15.6 mmol, 2 eq) were added to an ice-cooled solution of 5-methylisoxazole-3-carboxylic acid (990 mg, 7.8 mmol, 1 eq) in dichloromethane (80 ml), and stirring was carried out for 30 min. (R)-Methyl 3-amino-2,3-dihydro-1H-indene-5-carboxylate (A-07) (7.8 mmol, 1 eq) was dissolved in dichloromethane (20 ml) and added dropwise to the reaction solution, and stirring was carried out for 16 h at RT.The reaction solution was diluted with dichloromethane (250 ml), washed with sat. sodium hydrogen carbonate solution (50 ml), sat. ammonium chloride solution (50 ml), water (50 ml) and sat. NaCl solution (50 ml), dried over sodium sulfate and concentrated under reduced pressure.After purification by column chromatography (silica gel, 2percent MeOH in dichloro-methane), the desired product was obtained in the form of a yellowish solid. Yield: 68percent (1.6 g, 5.3 mmol).

3405-77-4 5-Methylisoxazole-3-carboxylic acid 76947, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; GRUENENTHAL GmbH; US2012/71461; (2012); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

3405-77-4, 5-Methylisoxazole-3-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,3405-77-4

(R)-Methyl 3-(5-methyl isoxazole-3-carboxamido)-2,3-dihydro-1H-indene-5-carboxylate (B-25)HATU (4.4 g, 11.7 mmol, 1.5 eq) and DIPEA (3.0 ml, 15.6 mmol, 2 eq) were added to an ice-cooled solution of 5-methylisoxazole-3-carboxylic acid (990 mg, 7.8 mmol, 1 eq) in dichloromethane (80 ml), and stirring was carried out for 30 min. (R)-Methyl 3-amino-2,3-dihydro-1H-indene-5-carboxylate (A-07) (7.8 mmol, 1 eq) was dissolved in dichloromethane (20 ml) and added dropwise to the reaction solution, and stirring was carried out for 16 h at RT.The reaction solution was diluted with dichloromethane (250 ml), washed with sat. sodium hydrogen carbonate solution (50 ml), sat. ammonium chloride solution (50 ml), water (50 ml) and sat. NaCl solution (50 ml), dried over sodium sulfate and concentrated under reduced pressure.After purification by column chromatography (silica gel, 2percent MeOH in dichloro-methane), the desired product was obtained in the form of a yellowish solid. Yield: 68percent (1.6 g, 5.3 mmol).

3405-77-4 5-Methylisoxazole-3-carboxylic acid 76947, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; GRUENENTHAL GmbH; US2012/71461; (2012); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

3405-77-4, 5-Methylisoxazole-3-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: N-protected-amino acid-OH or N-protected-peptide-OH (1?equiv) was dissolved in ? THF and cooled to??15?¡ãC. To the stirred solution, ? N-methylmorpholine (NMM) (1?equiv) and ? isobutylchloroformate (1?equiv) were added consecutively. After precipitation of ? N-methylmorpholine hydrochloride, the amine (1?equiv) was added and the mixture was allowed to warm to 25?¡ãC within 30?min. It was stirred for additional 90?min, and the solvent was removed under reduced pressure. The residue was dissolved in EtOAc and the solution was washed with H2O, saturated NaHCO3, 5percent citric acid and brine. The solvent was dried (MgSO4) and evaporated. The crude residue was purified by flash column chromatography to give the product.

3405-77-4, The synthetic route of 3405-77-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Chuck, Chi-Pang; Chen, Chao; Ke, Zhihai; Chi-Cheong Wan, David; Chow, Hak-Fun; Wong, Kam-Bo; European Journal of Medicinal Chemistry; vol. 59; (2013); p. 1 – 6;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

3405-77-4, 5-Methylisoxazole-3-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

The 470mg of compound 7 was dissolved in 2ml of dichloromethane was added 0.7mL TFA, stirred at room temperature for 2 to 4 hours, and after completion of the reaction, the solvent was distilled off under reduced pressure, drained oil pump, the oil was dissolved in 2mL of dichloromethane , and then added sequentially 0.8mL triethylamine, 0.11 g of0.14 g of of HOBT and 0.2g EDCI, the reaction system was stirred for 8 to 12 hours at room temperature, after completion of the reaction, successively with 1M hydrochloric acid, saturated sodium bicarbonate, saturated brine , organic phase was collected, dried over anhydrous sodium sulfate, and then filtered to remove the sodium sulfate, the organic phase was collected and the solvent was distilled off under reduced pressure, column chromatography on flash silica gel to give compound 9 0.41g, 85percent yield.

3405-77-4, As the paragraph descriping shows that 3405-77-4 is playing an increasingly important role.

Reference£º
Patent; Tianjin International Biology Medicine United Academe; Rao, Zihe; Fu, Cheng; Yang, Haitao; Yang, Cheng; Cai, Yan; Wang, Zhe; Liu, He; Li, shuang; (30 pag.)CN105837487; (2016); A;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

3405-77-4, 5-Methylisoxazole-3-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 111N-((ls,4s)-4-(2-(4′-(((3S,5R)-3,5-dimethylpiperazin-l-yl)methyl)biphenyl-3-yloxy)-5- fluoronicotinamido)cyclohexyl)-5-methylisoxazole-3-carboxamide HATU (0.104 g, 0.27 mmol) was added to a solution of 5-methylisoxazole-3-carboxylic acid (0.035 g, 0.27 mmol), N-((ls,4s)-4-aminocyclohexyl)-2-(4′-(((3S,5R)-3,5-dimethylpiperazin- l-yl)methyl)biphenyl-3-yloxy)-5-fluoronicotinamide (0.15 g, 0.25 mmol) and DIPEA (0.173 mL, 0.99 mmol) in DMF (5 mL) and the solution stirred at RT for 20 h. The mixture was purified by reverse phase HPLC with aqTFA/MeCN as eluant to the title compound as a white solid. Yield: 47 mg1U NMR (400 MHz, CD3OD) delta 8.45 (d, J = 7.9 Hz, IH), 8.11 (d, J = 3.4 Hz, IH), 8.07 (m, IH), 7.61 (d, J = 8.2 Hz, 2H), 7.49 (d, J = 5.3 Hz, 2H), 7.42 (m, 3H), 7.16 (m, IH), 6.38 (s, IH), 4.13 (m, IH), 3.94 (m, IH), 3.79 (s, 2H), 3.43 (m, 2H), 3.17 (m, 2H), 2.44 (s, 3H), 2.25 (m, 4H), 1.92 – 1.66 (m, 8H), 1.28 (d, J = 6.9 Hz, 6H). MS: APCI (+ve):641 (M+l)., 3405-77-4

3405-77-4 5-Methylisoxazole-3-carboxylic acid 76947, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2009/144494; (2009); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

3405-77-4, 5-Methylisoxazole-3-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(Step 1) Production of ethyl 3-(5-methyl-isoxazol-3-yl)-3-oxo-propionate To a suspension of 5-methyl-isoxazole-3-carboxylic acid (2.78 g) in tetrahydrofuran (20 mL) was gradually added CDI (3.60 g). After stirring at room temperature for 30 minutes, the reaction mixture was heated on an oil bath to 60¡ã C. After 1 hour, the reaction mixture was cooled to room temperature, magnesium chloride (2.30 g) was added followed by addition of ethyl potassium malonate (4.50 g). After stirring at room temperature for 3 hours, water (15 mL) was added to the reaction mixture followed by addition of 6 N hydrochloric acid (5.0 mL). The reaction mixture was concentrated, and the produced solid was collected by filtration, washed with water, and dried to obtain the title compound (3.99 g) as a white solid., 3405-77-4

3405-77-4 5-Methylisoxazole-3-carboxylic acid 76947, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; JAPAN TOBACCO, INC.; US2009/36450; (2009); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem