Heterocyclic Building Blocks-isoxazole

63366-79-0, Ethyl 3-methylisoxazole-5-carboxylate is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,63366-79-0

A round bottom flask with magnetic stirrer was charged with 3-methyl-isoxazole-5- carboxylic acid ethyl ester (900 mg, 5.8 mmol) in tetrahydrofuran (2.0 mL). To the reaction was added a solution of sodium hydroxide (465 mg, 11.6 mmol) in water (2 mL), followed by methanol (4 mL). The reaction was stirred at room temperature for 18 – 20 hours under an argon atmosphere. The reaction was transferred to a separatory funnel and the pH adjusted to 2 via addition of IN hydrochloric acid. The mixture was extracted with ethyl acetate (3 x 35 mL) and the combined extractions were washed with brine (1 x 50 mL), dried over magnesium sulfate, and filtered. The filtrate was concentrated in vacuo to yield S-methyl-isoxazole-S-carboxylic acid as a white solid (660 mg, 90percent). The solid was used without purification in the next reaction.

As the paragraph descriping shows that 63366-79-0 is playing an increasingly important role.

Reference£º
Patent; MILLENNIUM PHARMACEUTICALS, INC.; WO2006/91674; (2006); A1;,
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14678-02-5, 5-Amino-3-methylisoxazole is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixtureof CSA (23.2mg, 0.10mmol), 5-amino-3-methylisoxazole,(1.00mmol), isatin (1.00mmol), and -diketones(1.00mmol) in 5mL EtOH was irradiated with ultrasoundof low power at 70?C for the period of time indicated inScheme 2 and Table 3. After completion of the reaction, asindicated by TLC monitoring, the resultant solid was washedwith water and crystallized from ethanol to give productsa-d., 14678-02-5

14678-02-5 5-Amino-3-methylisoxazole 84590, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Article; Pelit, Emel; Journal of Chemistry; vol. 2017; (2017);,
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42831-50-5,42831-50-5, 5-Methylisoxazole-4-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 1.19: [4-(3-Chloro-phenylethynyl)-4-hvdroxy-piperidin-1-yl]-(5-methvl-isoxazol-4-v?- methanone; EPO MS (LC/MS): 345 [M+H]TLC Rf: 0.17 (EtOAc/cyclohex 1:1)

As the paragraph descriping shows that 42831-50-5 is playing an increasingly important role.

Reference£º
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2006/89700; (2006); 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.2510-36-3,3,5-Dimethylisoxasole-4-carboxylic acid,as a common compound, the synthetic route is as follows.

600 mg (4.3 mmol) 3,5-dimethyl-isoxazole-4-carboxylic acid were suspended in 5 ml. of toluene and two drops of dimethylformamide were added to the mixture. 0.39 ml. of thionylchloride (5.3 mmol) were added at room temperature and the reaction mixture was stirred at 65 0C for three hours. After removal of the solvent, toluene was added and the evaporation was repeated. The obtained residue was then dissolved in 5 ml. of dichloromethane and the solution was added dropwise to a solution containing 367 mg pyridazin-4-yl-amine (3.8 mmol) and 1.6 g (5.2 mmol) poly- merbound diisopropyl ethyl amine (PL-DIPAM resin, Polymer Laboratories) in 16 mL dichloromethane. The mixture was stirred for 16 h at room temperature. Then, the polymer was removed by filtration and washed with methanol. The solution that was obtained after washing contained 600 mg (58%, 90% purity) of the title compound which did not need further purification.

2510-36-3, As the paragraph descriping shows that 2510-36-3 is playing an increasingly important role.

Reference£º
Patent; BASF SE; VEZOUET, Ronan Le; SOeRGEL, Sebastian; DEFIEBER, Christian; GROss, Steffen; KOeRBER, Karsten; CULBERTSON, Deborah, L.; ANSPAUGH, Douglas, D.; WO2011/3793; (2011); A1;,
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946426-89-7, 5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazole-4-methanol is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

3-Chloro-4-bromophenol (3.8 g, 18.3 mmol) was mixed with (5-cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl)methanol (3.47 g, 12.2 mmol) and triphenylphosphine (6.41 g, 24.4 mmol) in toluene (150 mL). The mixture was cooled in an ice-bath and DIAD (4.8 mL, 24.4 mmol) as a solution in toluene (10 mL) was added drop-wise. The reaction was stirred at rt for 21 h and the solvents were removed on a rotavap leaving a yellow oily residue. This was dissolved in DCM (200 mL), silica (?20 g) was added and the mixture was evaporated to dryness. This material was loaded on the top of a silica column and purified eluting with hexanes/MTBE 9:1. The product containing fractions were pooled and the solvent removed under reduced pressure, leaving pure product 8e as a colourless oil that crystallized upon drying under vacuum overnight. Yield: 5.07 g (88%). H-NMR (CDCl3), delta (ppm): 7.45-7.30 (m, 4H), 6.90 (s, 1H), 6.60-6.55 (m, 1H), 2.15-2.07 (m, 1H), 1.32-1.25 (m, 2H), 1.20-1.11 (m, 2H), 946426-89-7

946426-89-7 5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazole-4-methanol 45790382, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; PHENEX PHARMACEUTICALS AG; Kinzel, Olaf; Steeneck, Christoph; Kremoser, Claus; US2014/221659; (2014); A1;,
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10557-85-4, 3,5-Dimethyl-4-iodoisoxazole is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

n-BuLi (1.6 M solution in hexanes, 6 mL, 9.6 mmol) was added to a cooled (-78C) solution of 4-iodo-3,5-dimethylisoxazole (1.47 g, 6.60 mmol) in TITF (24mL) under nitrogen. After 15 min, tributyllin chloride (26 mL, 9.60 mmol) was added and the reaction was stirred over night while warming to room temperature. The reaction was quenched by 1 M HC1, CH2C12 was added, the phases separated and the solvent were evaporated. The residue was purified by flash chromatography with heptane:CLI2Cl2 (75:25 – 0: 100) to give 3,5-dimethyl-4-(tributylstannyl)isoxazole (1.00 g, 39%).

10557-85-4, The synthetic route of 10557-85-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; KARO BIO AB; LOeFSTEDT, Joakim; WU, Xiongyu; KRUeGER, Lars; WO2011/42475; (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.3356-89-6,5-Chloro-3-phenylisoxazole,as a common compound, the synthetic route is as follows.

General procedure: To a stirred suspension of NaH (60% in mineral oil, 440 mg, 11 mmol, prewashed with hexane) in anhydrous THF (20 mL) was added the appropriate alcohol (15 mmol) at r.t. and the reaction mixture was stirred for 0.5 h. Next, 5-chloro-3-phenylisoxazole (2) (1.0 g, 5.6mmol) was introduced as a solid and the mixture was refluxed for 1 h. After cooling to r.t., the mixture was quenched with H2O (20 mL). For 4a and 4b, the resulting precipitate was collected, washed with H2O and recrystallized from hexane-Et2O mixture. For 3a, the reaction mixture was extracted with CH2Cl2 (3 ¡Á 20 mL). The combined organic layers were dried (Na2SO4) and concentrated in vacuo to give isoxazole 3a. 5-tert-Butoxy-3-phenylisoxazole (4c) was synthesized analogously using commercially available potassium tert-butoxide., 3356-89-6

The synthetic route of 3356-89-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Rostovskii, Nikolai V.; Agafonova, Anastasiya V.; Smetanin, Ilia A.; Novikov, Mikhail S.; Khlebnikov, Alexander F.; Ruvinskaya, Julia O.; Starova, Galina L.; Synthesis; vol. 49; 19; (2017); p. 4478 – 4488;,
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21169-71-1, Isoxazole-5-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: Compounds were synthesized in solution phase using Boc-protected amino acids on 100-200mg scale. Firstly, the amino acid (1.2-1.5equiv) was activated with HBTU (1.5equiv) and DIPEA (1.5equiv) as 0.2-0.5M solution in DMF for 10min. Then the solution was added to an amino group bearing C-terminal moiety (R1R2NH) and the mixture was stirred for a minimum of 1h at room temperature. The reaction mixture was diluted with EtOAc and washed with saturated NaHCO3 (2¡Á). The organic extracts were dried over MgSO4, filtered and evaporated in vacuo. The crude product was then treated with 20% TFA in DCM and stirred for 1-2h to remove the Boc group. TFA was removed by evaporating the reaction mixture under a stream of N2. The residue was dissolved in DCM and washed with saturated NaHCO3 (2¡Á). DCM phase was dried with MgSO4, filtered and evaporated in vacuo. Subsequent N-Boc-amino acids and amines were sequentially coupled under the same conditions. Each coupling reaction was monitored by ESMS, with most reactions going to completion overnight. All final compounds were purified on rpHPLC (97% by analytical HPLC) and fully characterized by NMR and HRMS (yields between 30% and 40%).

21169-71-1, 21169-71-1 Isoxazole-5-carboxylic acid 2060599, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Article; Yau, Mei-Kwan; Liu, Ligong; Lim, Junxian; Lohman, Rink-Jan; Cotterell, Adam J.; Suen, Jacky Y.; Vesey, David A.; Reid, Robert C.; Fairlie, David P.; Bioorganic and Medicinal Chemistry Letters; vol. 26; 3; (2016); p. 986 – 991;,
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Isoxazole | C3H3NO – PubChem

1072-67-9, 5-Methylisoxazol-3-amine is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 5-Methyl-3-aminoisoxazole (2 mmol) and aromatic aldehyde (2 mmol) were added to absolute ethanol (4~6 mL) with electromagnetic stirring for about 1 h, followed by adding p-nitroacetophenone (2 mmol) and concentrated HCl (0.1~0.2 mL) with continuous stirring. TLC monitored the reaction progress. Upon completion, the suspension was cooled overnight in a refrigerator (4C). The resulting solid was subsequently collected by filtration. The filter cake was washed successively with water (2×3 mL) and absolute ethanol (2×3 mL), dried to afford the corresponding crude product. The crude product was recrystallized in toluene or a mixed solvent of ethyl acetate and cyclohexane, dried in vacuum to give the pure product with 57.1% ~ 94.9% yields. All compounds were identified by 1H NMR, 13C NMR, ESI-MS and HR MS., 1072-67-9

1072-67-9 5-Methylisoxazol-3-amine 66172, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Article; Liu, Jinyu; Zhou, Zuwen; Liu, Jian; Yan, Jufang; Fan, Li; Tang, Xuemei; Liu, Jie; Chen, Feifei; Yang, Dacheng; Letters in drug design and discovery; vol. 16; 8; (2019); p. 835 – 845;,
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144537-05-3, N-Methyl-5-phenylisoxazole-3-carboxamide is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a solution of amide 3 (101 mg, 0.5 mmol) in THF (1 mL), asuspension of 60 wt % sodium hydride (100 mg, 2.5 mmol) inTHF (3 mL) was added under argon. After the mixture wasstirred vigorously for 10 min, the mixture was cooled to 0 Cand then a solution of tosyl chloride (191 mg, 1 mmol) in THF(1 mL) was slowly added. After the mixture was stirred for 3 hat 0 C, propylamine (164 muL, 2 mmol) was added, and then themixture was stirred at room temperature for 12 h. After evaporation of the solvent, the residue was dissolved into diethyl ether(5 mL), washed with water (5 mL), and the aqueous layer wasextracted with diethyl ether (2 ¡Á 5 mL). The combined organiclayer was dried over magnesium sulfate, and concentrated, andthe residue was subjected to column chromatography on silicagel to afford N-propylcarboxamide 5c (85 mg, 0.37 mol, 74%yield),

144537-05-3, 144537-05-3 N-Methyl-5-phenylisoxazole-3-carboxamide 10888957, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Article; Asahara, Haruyasu; Arikiyo, Keita; Nishiwaki, Nagatoshi; Beilstein Journal of Organic Chemistry; vol. 11; (2015); p. 1241 – 1245;,
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