Heterocyclic Building Blocks-isoxazole

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;,
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206055-91-6, (3-(4-Bromophenyl)isoxazol-5-yl)methanol is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 2: Preparation of (3-(4-(4,4,5,5-tetramethvI-l,3,2-dioxaboroIan-2- vI)phenvI)isoxazoI-5-yl)methanoI (llh)(3-(4-bromophenyl)isoxazol-5-yl)methanol (300 mg, 1.18 mmol), bis(pinacolato)diboron (750 mgs 3 mol), bis(diphenylphosphino)ferrocene dichloropalladium(193 mg, 0.24 mmol), and potassium acetate (348 mg, 3.54 mmol) were added to N,N- dimethylformamide (4 mL), followed by reaction at 90 C for 2 hours. After completion of the reaction was confirmed by TLC5 the reactants were filtered through celite. The filtrate was extracted with water (20 mL) and ethyl acetate (50 mL). The organic layer was washed with water (10 mL X 2) and brine (10 mL). The organic layer was separated, dried over anhydrous magnesium sulfate, and filtered under reduced pressure to remove ethyl acetate. The residue was purified by silica gel column chromatography using ethyl acetate and hexane as a developing solvent, thus affording the title compound (3-(4-(4,4,5,5-tetramethyl-l,3,2- dioxaborolan-2-yl)phenyl)isoxazol-5-yl)methanol (Hh). Yield: 60%.1U NMR(CDCl3, 400MHz): 7.88(d, 2H, J=8.0Hz), 7.79(d, 2H, J=7.6Hz), 6.58(s, IH), 4.81(s, 2H), and l.25(s, 12H)., 206055-91-6

As the paragraph descriping shows that 206055-91-6 is playing an increasingly important role.

Reference£º
Patent; DONG-A PHARM. CO., LTD.; YUHAN CO., LTD.; WO2008/108602; (2008); A1;,
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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.

62348-13-4, To a solution of CH3ONHCH3.HCl (780 mg) and acid chloride (19) in CH2Cl2 at 0 C. was added dry pyridine (1.35 ml) to afford a heterogenous mixture The solution was warmed to room temperature and stirred overnight. 1 M HCl was added to the reaction and the organic layer was separated, washed with brine, dried with Na2SO4, filtered, and concentrated in vacuo to give 1 g of product (85%).

As the paragraph descriping shows that 62348-13-4 is playing an increasingly important role.

Reference£º
Patent; Schering Corporation; US2004/106794; (2004); A1;,
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14441-90-8, 5-Phenylisoxazole-3-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Thionyl chloride (1.2 mL) was added at 0 C to the 3-phenylisoxazole-5-carboxylic acid 13 or the 5-phenylisoxazole-3-carboxylic acid 14 or the 5-(4-chlorophenyl)isoxazole-3-carboxylic acid 15 or the 3-(4-methylphenyl)isoxazole-5-carboxylic acid 16 (0.3 g, 1.58 mmol). The obtained suspension was stirred and heated at reflux for 16 h and then cooled at 0 C. At this temperature, a new addition of thionyl chloride (1.2 mL) was followed by another heating at reflux for 2 h. The reaction mixture was cooled at room temperature and the thionyl chloride excess was evaporated to dryness in vacuo. Anhydrous THF (2 mL) was added to the crude product. To the resulting solution, cooled at -5 C, was added dropwise a solution of appropriate amine (3.16 mmol) in dry THF (2 mL). The reaction mixture was stirred at room temperature for ca. 90 min (TLC, petroleum ether/ethyl acetate) and then the solid mass was filtered off and washed with THF. The filtrate was evaporated to dryness; the residue was treated with saturated sodium bicarbonate solution (20 mL) and extracted with dichloromethane (3¡Á15 mL). The combined organic phases were dried (Na2SO4) and evaporated to dryness to give the crude product, purified by flash-chromatography to give the desired amide., 14441-90-8

14441-90-8 5-Phenylisoxazole-3-carboxylic acid 151916, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Article; Cosimelli, Barbara; Simorini, Francesca; Taliani, Sabrina; La Motta, Concettina; Da Settimo, Federico; Severi, Elda; Greco, Giovanni; Novellino, Ettore; Costa, Barbara; Da Pozzo, Eleonora; Bendinelli, Sara; Martini, Claudia; European Journal of Medicinal Chemistry; vol. 46; 9; (2011); p. 4506 – 4520;,
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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

19788-36-4, The titled compound was prepared by the reaction of 2-chloro-3-(4-nitrophenyl)pyrazine (Step 1 of intermediate 11) (112 mg, 0.48 mmol) with (3,5-dimethylisoxazol-4-yl)methanol (61 mg, 0.48 mmol) using cesium fluoride (216 mg, 1.43 mmol) in DMSO (8.0 mL) as per the procedure described in Step 1 of Intermediate 51 to yield 109 mg of the product; 1H NMR (300 MHz, DMSO-d6) delta 2.22 (s, 3H), 2.45 (s, 3H), 5.33 (s, 2H), 8.22 (d, = 8.7 Hz, 2H), 8.32-8.38 (m, 3H), 8.43 (s, 1H).

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

Reference£º
Patent; GLENMARK PHARMACEUTICALS S.A.; DAS, Sanjib; GHARAT, Laxmikant Atmaram; HARDE, Rajendra Laxman; SHELKE, Sandeep Yadunath; PARDESHI, Shailesh Ramesh; THOMAS, Abraham; KHAIRATKAR-JOSHI, Neelima; SHAH, Daisy Manish; BAJPAI, Malini; (181 pag.)WO2017/21879; (2017); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.2552-54-7,3-(Benzyloxy)isoxazole-5-carboxylic acid,as a common compound, the synthetic route is as follows.

a) Synthesis of (3-benzyloxy-isoxazol-5-yl)-(2,3-dihydro-pyrido[4,3-b][1,4]oxazin-4-yl)-methanone To 10 ml of anhydrous tetrahydrofuran, 3-benzyloxy-isoxazol-5-carboxylic acid (50 mg, 0.23 mmol) and a catalytic amount of N,N-dimethyl formamide were added and dissolved, and then oxalyl chloride (35 mg, 0.28 mmol) was slowly added thereto and then stirred at room temperature for 4 hours. The reaction mixture was concentrated under reduced pressure. The residue was dissolved in dichloromethane, triethylamine (115 mg, 1.15 mmol) and 3,4-dihydro-2H-pyrido[4,3-b][1,4]oxazine (31 mg, 0.23 mmol) were added thereto and then stirred at room temperature for 2 hours. After completion of the reaction by adding water dropwise, the reaction mixture was extracted with dichloromethane, and the combined organic layer was dried over anhydrous sodium sulfate (Na2SO4), filtered and evaporated under reduced pressure. The residue was purified by column chromatography on amine silica eluding with a solvent of dichloromethane_methanol=30:1. The fractions containing the product were collected and evaporated to obtain (3-benzyloxy-isoxazol-5-yl)-(2,3-dihydro-pyrido[4,3-b][1,4]oxazin-4-yl)-methanone as pale-brown liquid (55 mg, 54% in two steps). 1H-NMR (CDCl3, 300 MHz); delta=8.23 (d, 1H, J=5.3 Hz), 7.32-7.48 (m, 6H), 6.87 (d, 1H, J=5.3 Hz), 6.52 (br s, 1H), 5.30 (s, 2H), 4.44 (m, 2H), 4.13 (m, 2H). MS (ESI); 338.1 (M++1).

2552-54-7, The synthetic route of 2552-54-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Ahn, Sung Oh; Park, Chan Hee; Im, Jun Hwan; Lee, Soon Ok; Lee, Kyoung June; Cho, Seong Wook; Ko, Kwang Seok; Han, Sun Young; Lee, Won Il; US2011/28467; (2011); A1;,
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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

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;,
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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;,
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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;,
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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;,
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