Heterocyclic Building Blocks-isoxazole

108511-97-3, Isoxazol-4-amine is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of methyl 2-(5-formyl-2-((2,2,2- trifluoroethyl)amino)pyrimidin-4-yl)-2-(4-methoxyphenyl)acetate (as prepared in General procedure III , Step G) (76 mg, 0.2 mmol, 1.0 equiv), isoxazol-4- amine (42 mg, 0.5 mmol, 2.5 equiv) in DCE/MeOH (3/0.5 mL) was added HOAc (42 mg, 0.7 mmol, 3.5 equiv). The mixture was stirred at 45 C overnight, then the mixture was cooled down to 0C, NaBH3CN (12 mg, 0.2 mmol, 1.0 equiv) was added to the reaction mixture in one portion, after which the resulting mixture was allowed to warm to room temperature and stirred for an additional l2h before being quenched with DCM (10 mL) and H2O (10 mL). The aqueous layer was extracted with DCM (10 mL x 3). The combined organic layers were dried over Na2S04 and concentrated. The residue was purified by Prep-TLC (PE:EA = 1/2) to give 6-(isoxazol-4-yl)-8-(4-methoxyphenyl)-2-((2,2,2- trifluoroethyl)amino)-5,6-dihydropyrido[-/, 3-6/]pyrimidin-7(-/r///)-one (51 mg, 44% yield) as a white solid. LC-MS: m/z 420 [M+H]+., 108511-97-3

As the paragraph descriping shows that 108511-97-3 is playing an increasingly important role.

Reference£º
Patent; AGIOS PHARMACEUTICALS, INC.; KONTEATIS, Zenon D.; LI, Mingzong; LIU, Peng; MEDEIROS, Matthew; REZNIK, Samuel K.; SUI, Zhihua; TRAVINS, Jeremy M.; POPOVICI-MULLER, Janeta; ZHOU, Shubao; MA, Guangning; (298 pag.)WO2019/191470; (2019); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

62348-13-4,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.62348-13-4,Isoxazole-5-carbonyl chloride,as a common compound, the synthetic route is as follows.

Compound 6 (14.21g, 30.39mmol) was added to absolute ethanol (150 mL), followed by gradual addition of isoxazol-5-carboxylic acid chloride (35mmol), stirring the reaction was warmed to reflux.After about 8 hours, the reaction was completed and TLC was used to monitor the end of the reaction.After the reactionsolution was allowed to stand for cooling, suction filtration, and the filter cake was washed with a small amount of anhydrous ethanol to obtain a white solid product N-(((4-(diphenyl[b,d]thiophen-3-yl)-7-) Oxy-2,2-dimethylpyridin-3-yl)methyl)sulfonyl)isoxazole-5-carboxamide, 15.73 g,yield 92%.

The synthetic route of 62348-13-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Zeng Qingqiang; (12 pag.)CN108586445; (2018); A;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

36958-61-9, 5-(Bromomethyl)-3-methylisoxazole is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A stirred suspension of12(1 g, 3.9 mmol), 5-(bromomethyl)-3-methyl-1,2-oxazole (0.48 mL, 4.3 mmol) and potassium carbonate (1.13 g, 8.2 mmol) in DMF (10 mL) was heated to 80 C for 4 h. After cooling to room temperature the reaction mixture was added to ice-water (100 mL) and stirred for 30 min. The resulting pink precipitate was collected by filtration to afford the title compound (0.89 g, 65%) as a pink powder. 1H NMR (300 MHz, DMSO-d6) delta 8.05-8.00 (m, 2H), 7.94-7.88 (m, 2H), 6.65 (s, 1H), 6.60 (s, 1H), 5.54 (s, 2H), 4.32 (q,J= 7.1 Hz, 2H), 2.25 (s, 3H), 1.31 (t,J= 7.1 Hz, 3H). LC-MS: (High pH) tR1.11 min,m/z351.2 [M-H]-, 96% purity, 36958-61-9

As the paragraph descriping shows that 36958-61-9 is playing an increasingly important role.

Reference£º
Article; Mould, Daniel P.; Bremberg, Ulf; Jordan, Allan M.; Geitmann, Matthis; Maiques-Diaz, Alba; McGonagle, Alison E.; Small, Helen F.; Somervaille, Tim C.P.; Ogilvie, Donald; Bioorganic and Medicinal Chemistry Letters; vol. 27; 14; (2017); p. 3190 – 3195;,
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Isoxazole | C3H3NO – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.3209-71-0,Isoxazole-3-carboxylic Acid,as a common compound, the synthetic route is as follows.

Amine 32-1 (73 mg, 0.209 mmol) was added to anhydrous dimethylformamide (2.0 mL). Isoxazole-3-carboxylic acid (23.6 mg, 0.209 mmol), EDC (40.1 mg, 0.209 mmol), HOBT (32 mg, 0.209 mmol) and triethylamine (58 0.418 mmol) were added sequentially and the resulting reaction mixture was allowed to stir at room temperature for 18 h. Following this duration, the contents were filtered and the resulting filtrate was purified via reverse-phase HPLC (5-95%, 0.1% TFA in H20:acetonitrile) to give 32-2 as a white solid. MS m/z (M+H): calculated = 445.1794; observed = 445.1808. NMR delta (ppm)(CHCl3-d): 8.50-8.43 (1 H, m), 7.14 (1 H, d, J = 8.42 Hz), 6.79-6.75 (1 H, m), 6.03 (1 H, d, J = 8.47 Hz), 5.10-5.01 (2 H, m), 4.18-4.08 (2 H, m), 3.90 (1 H, dd, J = 13.05, 3.18 Hz), 3.83-3.66 (3 H, m), 3.58-3.50 (1 H, m), 3.41 (3 H, d, J = 10.20 Hz), 2.15 (2 H, t, J = 14.76 Hz), 1.96 (4 H, d, J = 20.07 Hz).

3209-71-0, 3209-71-0 Isoxazole-3-carboxylic Acid 11286453, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; LAYTON, Mark, E.; PERO, Joseph, E.; RODZINAK, Kevin, J.; ROSSI, Michael, A.; WO2011/34741; (2011); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1228690-37-6,(R)-1-Phenylethyl (5-(4-bromophenyl)-3-methylisoxazol-4-yl)carbamate,as a common compound, the synthetic route is as follows.

To a stirred solution of III-3 (190.9 mg, 0.64 mmol), III-4 (290.7 mg, 0.72 mmol), Na2CO3 (128.1 mg, 1.21 mmol) in DME/H2O (20 mL, v/v=3:1) was added Pd(dppf)Cl2 (66.4 mg, 0.09 mmol) under nitrogen. Then the solution was heated to reflux for 4 hours. After concentrated, H2O (5 mL) was added, and the mixture was extracted with EtOAc. The organic layer was combined and washed with brine, dried over Na2SO4, concentrated in vacuo. The residue was purified by column chromatography on silica gel (PE:EA=1:1) to afford III-5 (256 mg, yield: 26.9%)., 1228690-37-6

1228690-37-6 (R)-1-Phenylethyl (5-(4-bromophenyl)-3-methylisoxazol-4-yl)carbamate 66660383, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; Buckman, Brad Owen; Nicholas, John Beamond; Emayan, Kumaraswamy; Seiwert, Scott D.; US2014/200215; (2014); 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

42831-50-5, 5-Methylisoxazole-4-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 5-methylisoxazole-4-carboxylic acid SM (500 mg, 4.0 mmol) in toluene(10 mL) was added SOd2 (720 mg, 6.0 mmol). The mixture was heated to reflux for 3 hours. Thereaction mixture was concentrated under reduced pressure to obtain 5-methylisoxazole-4-carbonyl chloride compound 1 (550 mg, crude) without further purification.

42831-50-5, 42831-50-5 5-Methylisoxazole-4-carboxylic acid 1425240, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; ABBVIE INC.; MICHAELIDES, Michael; HANSEN, Todd; DAI, Yujia; ZHU, Guidong; FREY, Robin; GONG, Jane; PENNING, Thomas; CURTIN, Michael; MCCLELLAN, William; CLARK, Richard; TORRENT, Maricel; MASTRACCHIO, Anthony; KESICKI, Edward A.; KLUGE, Arthur F.; PATANE, Michael A.; VAN DRIE, John H. Jr.; JI, Zhiqin; LAI, Chunqiu C.; WANG, Ce; (1190 pag.)WO2016/44770; (2016); 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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.21080-81-9,Ethyl 5-cyclopropylisoxazole-3-carboxylate,as a common compound, the synthetic route is as follows.

[0266] Into a 10-L round-bottom flask was placed ethyl 5-cyclopropylisoxazole-3- carboxylate (280 g, 1.55 mol, 1.00 equiv) and a solution of sodium hydroxide (74.3 g, 1.20 equiv) in water (4 L). The resulting solution was stirred for 1 h at room temperature. The resulting mixture was washed with ether. The pH value of the aqueous solution was adjusted to 2-3 with hydrochloric acid (12N). The resulting solution was extracted with ethyl acetate and the organic layers combined and concentrated under vacuum. This resulted in 220 g (93%>) of 5-cyclopropylisoxazole-3-carboxylic acid as an off- white solid. 1H-NMR (300 MHz CDC13): delta 8.42 (brs, 1H), 6.37 (s, 1H), 2.16-2.05 (m, 1H), 1.29-1.12 (m, 2H), 1.12-0.99 (m, 2H); LCMS m z = 153.9 [M+H]+., 21080-81-9

The synthetic route of 21080-81-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; EPIZYME, INC.; FOLEY, Megan Alene Cloonan; KUNTZ, Kevin Wayne; MILLS, James Edward John; MITCHELL, Lorna Helen; MUNCHHOF, Michael John; HARVEY, Darren Martin; (208 pag.)WO2016/40498; (2016); A1;,
Isoxazole – Wikipedia
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19788-36-4, (3,5-Dimethyl-4-isoxazolyl)methanol is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(3,5-Dimethylisoxazol-4-yl)methanol (0.28 g, 1.5 mmol), methyl (2S)- 2-(1 ,3-benzoxazol-2-ylamino)-3-(4-hydroxyphenyl)propionate (0.31 g, 1 mmol) and triphenylphosphine (0.26 g, 1 mmol) were dissolved in 5 ml of tetrahydrofuran (THF). The reaction mixture was cooled to 5C. DEAD (0.52 g, 3 mmol) was then added and the reaction was stirred at room temperature for 18-24h. Subsequently, THF was evaporated to obtain the product, the title acid methyl ester. The crude product was dissolved in a THF/MeOH/H2O mixture(6:0.1 :1 , 2 ml). 1M LiOH (1.6 ml) was added and the reaction was stirred for 3 days at room temperature. Then the reaction mixture was neutralized with 1M HCl, a small amount of water was added and the mixture extracted with ethyl acetate. The solvent was evaporated. The purification was performed by chromatography. The yield was 60%. MS (ES) 407 (M+, 100%), 19788-36-4

As the paragraph descriping shows that 19788-36-4 is playing an increasingly important role.

Reference£º
Patent; ADAMED SP. Z O.O.; WO2006/67086; (2006); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem