Day: September 30, 2020

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

N-(2,4-dimethylphenyl)-3-hydroxy-N-isobutylbenzenesulfonamide (76.9 mg, 0.231 mmol), (3,5- dimethylisoxazol-4-yl)methanol (36.7 mg, 0.288 mmol) and (4-(3,3,4,4,5,5,6,6,7,7,8,8,9,9, 10, 10, 10-heptadecafluorodecyl)phenyl)diphenylphosphine (204 mg, 0.288 mmol) were added to a 2-5mL Biotage microwave vessel. Tetrahydrofuran (THF) (4 mL) was added followed by diisopropyl diazene-l,2-dicarboxylate (DIAD) (0.056 mL, 0.288 mmol). The reaction vial was sealed and left to stir overnight at RT. The reaction mixture was concentrated in vacuo and then diluted with ethyl acetate (25mL) and water (25mL). The organic fraction was separated, dried and then concentrated in vacuo to give the crude product. The crude product was dissolved in DMF: H20 (9: 1) ImL, and loaded onto a flurous column(preconditioned with ImL DMF, followed by 6mL MeOH: H20 (5: 1). The semi purified fraction was eluted with 6mL MeOH: H20 (5: 1). The fraction was concentrated down, and dissolved in 1: 1 MeOH:DMSO 1 mL and purified by mass directed autoPrep on Sunfire C18 column usingAcetonitrile Water with a Formic acid modifier. The solvent was dried under a stream of nitrogen in the Radleys blowdown apparatus to give the required product, 37.7 mg., 19788-36-4

The synthetic route of 19788-36-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXO GROUP LIMITED; BIRAULT, Veronique; CAMPBELL, Amanda, Jennifer; HARRISON, Stephen; LE, Joelle; WO2013/45431; (2013); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

954230-39-8,954230-39-8, Ethyl 3-(4-fluorophenyl)-5-methylisoxazole-4-carboxylate is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step d: r3-(4-Fluoro-phenyl)-5-methyl-isoxazol-4-yll-methanol: To a solution of 3-(4-fluoro-phenyl)-5-methyl-isoxazole-4-carboxylic acid ethyl ester (3.0 g, 12 mmol) (6.18 g, 25 mmol) in THF (320 mL) was added portionwise lithiumaluminiumhydride (528 mg, 14 mmol) at 0 C and the reaction mixture was stirred at room temperature for 3 h. The mixture was then cooled to 0 C and water (518 mul) added followed by sodium hydroxide (15% solution, 518 mul) and then again water (1.5 mL) and the mixture then stirred overnight at room temperature. The precipitate was then filtered off and washed with THF. The combined washings and filtrate were then evaporated. Purification by chromatography (Si02, heptane:ethyl acetate = 100:0 to 1: 1) afforded the title compound (1.8 g, 71%) which was obtained as a white solid. MS: m/e = 208.1 [M+H]+.

As the paragraph descriping shows that 954230-39-8 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.108511-97-3,Isoxazol-4-amine,as a common compound, the synthetic route is as follows.

To a solution of 4-aminoisoxazole (2.00 g, 23.79 mmol; CASNo. 108511-97-3) in THF (50 mL) at 0 0C was added pyridine (1.92 mL, 23.79 mmol,) followed by phenyl chloroformate (3.28 mL, 26.17 mmol,). After stirring at 0 0C for 2.5 h, the reaction was warmed to room temp overnight. The reaction was diluted with ethyl acetate and washed with 2M HCI, water, saturated sodium bicarbonate, and brine. The organic layer was dried over magnesium sulfate, filtered, concentrated, and purified by flash chromatography (dichloromethane/hexane) to give the title compound as a white solid (2.07 g, 10.15 mmol, 50%)., 108511-97-3

108511-97-3 Isoxazol-4-amine 13804278, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; PFIZER INC.; WO2009/127948; (2009); A1;; ; Patent; PFIZER INC.; WO2009/127949; (2009); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

62348-13-4,62348-13-4, Isoxazole-5-carbonyl chloride is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 3-(5-(aminomethyl)-2-chlorophenyl)-1-(4-(trifluoromethyl)phenyl)-1H- 1,2,4-triazol-5(4H)-one (Intermediate-63, 0.060 g, 0.162 mmol) in dry THF ( 5 mL) was added DIPEA (3 mL) and stirred for 20 minutes. The reaction mixture was cooled to 0C and isoxazole-5-carbonyl chloride (0.032 g, 0.243 mmol) was added and stirred for 3 h at room temperature. The reaction mass was quenched in water, extracted with DCM: MeOH and concentrated to afford crude product which was purified by column chromatography eluting with MeOH: DCM to afford 0.030 g of pure product. 1H NMR (400 MHz, DMSO d6): delta 4.50-4.52 (d, J = 8Hz, 2 H), 7.09-7.10 (d, = 2 Hz, 1H), 7.43- 7.45 (d, J = 8.4 Hz, 1H), 7.50-7.53 (d, J = 10.4Hz, 1H), 7.59-7.64 (d, J= 18 Hz, 1H), 7.82-7.85 (d, / = 8.8 Hz, 2H), 8.17-8.19 (d, J = 8.4 Hz, 2H), 8.74-8.75 (d, J – 2Hz, 1H), 9.58-9.61 (t, 1H), 12.61-12.74 (br s, 1H); MS (m/z): 464.11 (M+H+).

62348-13-4 Isoxazole-5-carbonyl chloride 2736707, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; GLENMARK PHARMACEUTICALS S.A.; GHARAT, Laxmikant Atmaram; MUTHUKAMAN, Nagarajan; KHAIRATKAR-JOSHI, Neelima; KATTIGE, Vidya Ganapati; WO2013/186692; (2013); 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.36958-61-9,5-(Bromomethyl)-3-methylisoxazole,as a common compound, the synthetic route is as follows.

Sodium hydride (60% w/w) (34.1 mg, 0.85 mmol) was added to a stirring solution of 7-benzylsulfanyl-4-(cyclopropanecarbonyl)-2H-isoquinolin-1 -one (220. mg, 0.66 mmol) in DMF (8 mL). After 15 min 5-(bromomethyl)-3-methyl-1 ,2-oxazole (0.15 mL, 0.85 mmol) was added and the reaction mixture stirred at ambient temperature for 1 h. DCM (25 mL) and saturated aq. NaHC03 (25 mL) were added and the mixture stirred for 5 min. The DCM layer was isolated by passing through a hydrophobic frit and the aqueous layer washed with DCM. The combined DCM extracts were concentrated under reduced pressure and purified by automated column chromatography, SiO2, eluent 0-100% EtOAc in iso- Hexane to yield 7-benzylsulfanyl-4-(cyclopropanecarbonyl)-2-[(3-methylisoxazol-5- yl)methyl]isoquinolin-1 -one (263 mg, 0.61 mmol, 93%). Used directly in the synthesis of Intermediate S10-C1, 36958-61-9

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

Reference£º
Patent; CANCER RESEARCH TECHNOLOGY LIMITED; MCGONAGLE, Alison E.; JORDAN, Allan; WASZKOWYCZ, Bohdan; HUTTON, Colin; WADDELL, Ian; HITCHIN, James R.; SMITH, Kate Mary; HAMILTON, Niall M.; (497 pag.)WO2016/92326; (2016); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

59669-59-9,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.59669-59-9,3-(tert-Butyl)isoxazol-5-amine,as a common compound, the synthetic route is as follows.

To a cold slurry of (S)-1-(4-Chloro-phenyl)-4-oxo-azetidine-2-carboxylic acid (0.2g; 1.037mmol) and 5-amino-3-tert-butylisoxazole (0.145g; 1.037mmol) in pyridine (1.258mL; 15.555mmol) is added phosphorous oxychloride (O.l lbetamL; 1.244mmol). The mixture is stirred at O¡ãC for 30 minutes and then diluted with water and extracted with ethyl acetate several times. The organics are combined and washed with water and brine, dried over Na2SO4, filtered and concentrated in vacuo. Purification by preparative HPLC affords title compound, m/z 348 [M+H+]

The synthetic route of 59669-59-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; HICKEY, Eugene, Richard; RIETHER, Doris; THOMSON, David, Smith; WU, Lifen; ZINDELL, Renee, M.; WO2010/147791; (2010); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

21169-71-1, Isoxazole-5-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

21169-71-1, General procedure: To a solution of the benzoxazole core (1.0 eq) in DCM (2 mL) was added the carboxylic acid (1.2 eq), EDCI (1.2 eq) and DMAP (0.1 eq). The solution was stirred under nitrogen at 45 C overnight. Work-up 1 (W1): The solution was extended with DCM, a saturated solution of sodium bicarbonate was added and the mixture was extracted three times with DCM. The combined organic layers were then washed with brine, dried with sodium sulphate and the solvent was removed in vacuo. Purification by column chromatography on silica gel, eluting ethyl acetate/cyclohexane 50:50 led to the desired carboxamide.

The synthetic route of 21169-71-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Ferrins, Lori; Rahmani, Raphael; Sykes, Melissa L.; Jones, Amy J.; Avery, Vicky M.; Teston, Eliott; Almohaywi, Basmah; Yin, JieXiang; Smith, Jason; Hyland, Chris; White, Karen L.; Ryan, Eileen; Campbell, Michael; Charman, Susan A.; Kaiser, Marcel; Baell, Jonathan B.; European Journal of Medicinal Chemistry; vol. 66; (2013); p. 450 – 465;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

288-14-2, Isoxazole is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General Procedure 49 Isoxazole (0.64 mL, 10 mmol) was added to a solution of N-iodosuccinimide (2.3 g, 10 mmol) in trifluoroacetic acid (20 mL). After stirring overnight, water (50 mL), hexanes (50 mL) and sodium bisulfite were added to the reaction. The phases were separated and the organic phase was dried over Na2SO4, filtered and concentrated by rotary evaporation to give 4-iodo-isoxazole (218 mg, 11%).

288-14-2, As the paragraph descriping shows that 288-14-2 is playing an increasingly important role.

Reference£º
Patent; AGOURON PHARMACEUTICALS, INC.; US2006/46991; (2006); 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

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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1083224-23-0,5-(2,4-Difluorophenyl)isoxazole-3-carboxylic acid,as a common compound, the synthetic route is as follows.,1083224-23-0

[0301] To a solution of 5 -(2, 4-difluorophenyl)isoxazole-3 -carboxylic acid (100 mg, 0.44 mmol, 1 equiv) in DMF (1 mL), were added HATU (185 mg, 0.48 mmol, 1.1 equiv). The mixture was treated drop wise with DIPEA (183 mg, 1.42 mmol, 3.2 equiv). After stirring at RT for 15 minutes, the mixture was treated drop wise with a solution of the l-(2,4- bis(trifluoromethyl)benzyl)-lH-pyrazol-4-amine (137 mg, 0.44 mmol, 1 equiv) in DMF (1 mL). The reaction mixture was kept under stirring for 24 hrs at RT. Product formation was confirmed with TLC & LCMS and reaction mixture was diluted EtOAc (50 mL) & washed with water (50 mL X 2). Organic layer dried over Na2S04 & concentrated under reduced pressure to obtain crude which was further purified by flash column chromatography to obtain pure product N-(l-(2,4-bis(trifluoromethyl)benzyl)-lH-pyrazol-4-yl)-5-(2,4- difluorophenyl)isoxazole-3-carboxamide. (36 mg, 15.7% as off white solid) ‘fl NMR (400 MHz, DMSO-c 6) d 11.16 (s, 1H), 8.33 (s, 1H), 8.10 (q, J= 8.3 Hz, 3H), 7.78 (s, 1H), 7.6l(t, J= 10.9 Hz, 1H), 7.35 (dd, J= 10.1, 7.7 Hz, 1H), 7.26 (d, J= 2.9 Hz, 1H), 7.06 (d, J= 8.1Hz, lH),5.67 (s, 2H).

The synthetic route of 1083224-23-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PRAXIS BIOTECH LLC; ALFARO, Jennifer; BELMAR, Sebastian; NUNEZ VASQUEZ, Gonzalo Esteban; PUJALA, Brahmam; SATHE, Balaji Dashrath; BERNALES, Sebastian; CHAKRAVARTY, Sarvajit; THAKRAL, Pooja; PATIDAR, Rajesh Kumar; (344 pag.)WO2019/195810; (2019); A2;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem