Tag: M.W:0-100

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.300-87-8,3,5-Dimethylisoxazole,as a common compound, the synthetic route is as follows.

Intermediate 1 : 4-iodo-3,5-Dimethylisoxazole; Nitric acid (13ml) was added dropwise (exothermic reaction) to a mixture of 3,5- dimethylisoxazole (31.3g, 320mmol) and iodine (37.3g, 150 mmol) and the mixture was stirred at room temperature for 1 h. The reaction mixture was hydrolysed with a mixture of ice and water and extracted with DCM. The organic phase was washed with a solution of Na2S203, dried over Na2S04 and concentrated under reduced pressure to afford the title compound as a yellow solid (60g, 83%). [APCI MS] m/z: 224 MH+, Rt 2.17min., 300-87-8

The synthetic route of 300-87-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXOSMITHKLINE LLC; BOUILLOT, Anne, Marie, Jeanne; DONCHE, Frederic; GELLIBERT, Francoise, Jeanne; LAMOTTE, Yann; MIRGUET, Olivier; WO2011/54846; (2011); 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.14678-05-8,Isoxazol-5-amine,as a common compound, the synthetic route is as follows.

Example 26-Methyl-4-(3-methyl-lH-indazol-5-yl)-4,7-dihydroisoxazolo[5,4-b]pyridine-5-carbonitrileA mixture of 50 mg (0.22 mmol) (2?)-2-[(3-methyl-lH-indazol-5-yl)methylidene]-3-oxobutane- nitrile (Example 2A) and 19 mg (0.22 mmol) 1 ,2-oxazol-5-amine in propan-2-ol (1.0 ml) was stirred at reflux temperature overnight. The reaction mixture was then concentrated under reduced pressure, and the residue was purified by preparative RP-EtaPLC (acetonitrile/water + 0.1% TFA gradient) to yield 45 mg (69% of th.) of the racemic title compound.LC-MS (method 2): R, = 0.85 min; MS (ESIpos): m/z = 292 (M+Eta)+ 1H-NMR (400 MHz, DMSOd6): delta = 12.63 (br. s, IH), 10.91 (s, IH), 8.14 (s, IH), 7.55 (s, IH), 7.43 (d, IH), 7.19 (d, IH), 5.02 (s, IH), 2.48 (s, 3H), 2.16 (s, 3H) ppm., 14678-05-8

The synthetic route of 14678-05-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BAYER SCHERING PHARMA AKTIENGESELLSCHAFT; MICHELS, Martin; FOLLMANN, Markus; VAKALOPOULOS, Alexandros; ZIMMERMANN, Katja; TEUSCH, Nicole; LOBELL, Mario; WO2011/3604; (2011); 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.

General procedure: N-protected amino acid was dissolved in dichloromethane (DCM). 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC.HCl, 1.3 eq.) and hydroxybenzotriazole (HOBt ¡¤xH2O, 1.3 eq.) were added at 0 C and the mixture was stirred for 50 min, after which thecorresponding amine (1.3 eq.) and N,N-Diisopropylethylamine (DIPEA, 1.3 eq.) were added at 0C. After stirring overnight, the mixture was washed with a 5% potassium sulfate solution(KHSO4), a 5% sodium bicarbonate solution (NaHCO3) and with water. After drying over sodiumsulfate (Na2SO4) and evaporation of the solvent, the residue was purified via columnchromatography., 108511-97-3

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

Reference£º
Article; Silva, Daniel G.; Ribeiro, Jean F.R.; De Vita, Daniela; Cianni, Lorenzo; Franco, Caio Haddad; Freitas-Junior, Lucio H.; Moraes, Carolina Borsoi; Rocha, Josmar R.; Burtoloso, Antonio C.B.; Kenny, Peter W.; Leitao, Andrei; Montanari, Carlos A.; Bioorganic and Medicinal Chemistry Letters; vol. 27; 22; (2017); p. 5031 – 5035;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.16401-14-2,Isoxazole-5-carbaldehyde,as a common compound, the synthetic route is as follows.

General procedure: A solution of 19 (300 mg, 0.70 mmol) in tetrahydrofuran (3 mL) was slowly added to a solution of lithium diisopropylamide (LDA) in heptane/tetrahydrofuran/ethylbenzene (2 M, 0.38 mL, 0.76 mmol) at 78oC, and the resultant solution was stirred at -78oC for 30 minutes. Chlorotitanium triisopropoxide (1 M, 2.8 mL) was then added slowly, and the resulting mixture was stirred at 40oC for 1 hour. The reaction was cooled to -78oC, and propionaldehyde (49 mg, 0.84 mmol) was added slowly. This mixture was then warmed to 40oC, and stirred at 40oC for 2 hours. The reaction mixture was quenched with saturated aqueous ammonium chloride solution (1 mL), diluted with 10 mL of tetrahydrofuran, and treated with Celite for 1 hour. The resultant slurry was filtered and concentrated. The resultant residue was purified by silica gel chromatography (gradient: 95:5 hexanes:ethyl acetate to 65:35 hexanes:ethyl acetate) to provide 20 as a white solid. Yield: 230 mg, 68%., 16401-14-2

The synthetic route of 16401-14-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Warmus, Joseph S.; Quinn, Cheryl L.; Taylor, Clarke; Murphy, Sean T.; Johnson, Timothy A.; Limberakis, Chris; Ortwine, Daniel; Bronstein, Joel; Pagano, Paul; Knafels, John D.; Lightle, Sandra; Mochalkin, Igor; Brideau, Roger; Podoll, Terry; Bioorganic and Medicinal Chemistry Letters; vol. 22; 7; (2012); p. 2536 – 2543;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5765-44-6,5-Methylisoxazole,as a common compound, the synthetic route is as follows.,5765-44-6

In 50 ml double-mouth bottle is added sodium hydroxide (0.24 g, 6.0 mmol) and anhydrous methanol (10 ml), in the 30 C dropping under 5 – methyl isoxazole (0.49 ml, 6.0 mmol), then stir at room temperature overnight. Steams solvent, the residue with ethyl ether (80 ml) washing, filtering, the filter cake by vacuum drying to obtain a white solid (0.57 g, 90%).

The synthetic route of 5765-44-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Guangdong Dongyangguang Pharmaceutical Co., Ltd.; Wang Xiaojun; Zuo Yinglin; Yang Chuanwen; Wang Jiancheng; Wang Hui; (26 pag.)CN109721536; (2019); A;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.354795-62-3,3-Methylisoxazol-4-amine,as a common compound, the synthetic route is as follows.

A mixture of 2-[(phenylmethyl)oxy]-5-(4-pyridinyl)benzoic acid (may be prepared as described in Description 79; 0.12 g, 0.36 mmol), EDC (0.14 g, 0.72 mmol) and HOBT (0.11 g, 0.72 mmol) in Nu,Nu-dimethylformamide (2 ml) was stirred in air at room temperature for 1 h, then 3-methyl-4-isoxazolamine (may be prepared as described in Description 91; 100 mg, 1.02 mmol) was added in one charge. The reaction mixture was stirred at 25 C overnight. The reaction mixture was diluted with water (25 ml). The solid was filtered, washed with water (30 ml) and methanol (5 ml x 2), and dried in vacuo to yield the title compound as a grey solid. 72 mg.1HNMR (400 MHz, DMSO- /6): 9.97 (s, 1 H), 9.19 (s, 1 H), 8.63 (d, 2H, J=6.0), 8.18 (d, 1 H, J=2.4), 8.04 (dd, H, J=2.4, J=8.8), 7.75 (d, 2H, J=6.0), 7.56 (d, 2H, J=6.8),7.49-7.38 (m, 4H), 5.34 (s, 2H), 1.95 (s, 3H).MS (electrospray): m/z [M+H]+ = 386.00, 354795-62-3

The synthetic route of 354795-62-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLAXO GROUP LIMITED; GLAXOSMITHKLINE (CHINA) R&D COMPANY LIMITED; NICHOLS, Paula Louise; EATHERTON, Andrew John; BAMBOROUGH, Paul; JANDU, Karamjit Singh; PHILPS, Oliver James; ANDREOTTI, Daniele; WO2011/38572; (2011); 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.87988-94-1,5-Methylisoxazol-4-amine,as a common compound, the synthetic route is as follows.,87988-94-1

Example 8(a) 5-Acetyl-l-(tetrahydro-2H-pyran-4-yl)- 2-trifluoromethyl-lH-imidazole; 5-Methyl-4-amino-isoxazole (1.7 g, 17.25 mmol) and acetic acid (1.1 g, 19 mmol) were dissolved in methanol (50 mL). Tetrahydro-2H-pyran-4-one (1.9 g, 19 mmol) was added and the mixture was cooled to 0 – (-5) 0C and stirred for 1 h. Sodium cyanoborohydride (0.812 g, 12.9 mmol) was added in portions to the reaction mixture at -5 C, causing weak exothermic and gas evolution. The cooling bath was removed and the mixture was stirred at r.t. for 2 h followed by addition of water (20 mL). The methanol was removed from the reaction mixture, and the intermediate amine was extracted with ethyl acetate (3×80 mL). The combined organic layers were dried (Na2SO4), concentrated to dryness, dissolved in toluene and re-concentrated. The crude intermediate amine, was dissolved in CH2Cl2 (20 mL) and pyridine (2 mL, 26 mmol) was added. The mixture was cooled to 0C and trifluoroacetic anhydride (4.35 g, 20.7 mmol) was added dropwise. The mixture was continued stirring for 2 h at r.t. and was then washed with water and saturated NaHCO3. The aqueous layer was extracted with CH2Cl2 (2×30 mL), the organic extracts were dried (Na2SO4) and concentrated to dryness to give a second crude intermediate, 4-[N- (tetrahydro-2H-pyran-4-yl)]-N-trifluoroacetyl-amino-5-methylisoxazole. MS (ES) m/z 279 (M++.). The title compound was prepared in accordance with the general method of Example 6 (b) using the intermediate 4-[N-(tetrahydro-2H-pyran-4-yl)]-N-trifluoroacetyl- amino-5-methylisoxazole (max 17.25 mmol), with the exception that the product was purified by flash chromatography (heptane/EtOAc 3:2), giving the title compound (3.03 g, 67%).1H nuMR (CDCl3, 300 MHz) delta 7.85 (s, 1 H), 4.89-4.75 (m, 1 H), 4.17-4.07 (m, 2 H), 3.54- 3.44 (m, 2 H), 2.75-2.60 (m, 2 H), 2.56 (s, 3 H), 1.72-1.63 (m, 2 H); MS (ES) m/z 263 (M+l).

87988-94-1 5-Methylisoxazol-4-amine 13033202, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; ASTRAZENECA AB; WO2008/2244; (2008); A2;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

5765-44-6, 5-Methylisoxazole is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5765-44-6

Sodium (7.36 g, 320 mmol) was reacted with ethanol (368 ml) and then 5-methylisoxazole (26.56 g, 320 mmol) was added to the mixture at 20 C. The mixture wasstirred at 20 oc for 1.5 h and at 0 oc for 1.5h. The white solid was collected by filtration,washed with ether, dried in vacuo to provide the titled compound (1 0.168 g, 30%) as awhite solid.

As the paragraph descriping shows that 5765-44-6 is playing an increasingly important role.

Reference£º
Patent; GLAXOSMITHKLINE LLC; LIN, Hong; MOORE, Michael Lee; QU, Junya; RIVERO, Ralph A.; TEDESCO, Rosanna; YU, Hongyi; LUENGO, Juan Ignacio; WO2013/28263; (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.108511-97-3,Isoxazol-4-amine,as a common compound, the synthetic route is as follows.

Dissolving 1-chloro-4-iodo-2-trifluoromethylbenzene (10 mmol) obtained in Reaction 1.220 ml of toluene,Isoxazole-4-amine is added sequentially to the system(12mmol),Palladium acetate (0.5 mmol),2,2′-bis(diphenylphosphino)-1,1′-binaphthyl(12 mmol), 3 ml of triethylamine, after stirring for 10 minutes, add 10 ml of cesium carbonate (10 mmol)The aqueous solution is heated to 50 C for 4 hours. After the reaction is completed, 20 ml of water is added to the system.Stir for 20 minutes, dispense,The organic phase is dried over anhydrous sodium sulfate. Concentrated, flash column chromatography,2.2 g of yellow N-(4-chloro-3-trifluoromethylphenyl)-isoxazole-4-amine powder was obtained with a yield of 84%.

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

Reference£º
Patent; Zhang Ruwei; Ge Baoyin; Jing Fan; (7 pag.)CN108432776; (2018); A;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

98019-60-4, Isoxazol-5-ylmethanol is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,98019-60-4

Step 2Isoxazole-5-carbaldehydeIn a round-bottomed flask, isoxazol-5-yl-methanol (511 mg, 5.16 mmol) was dissolved in dichloromethane (30 ml). Dess-Martin periodinane (2.3 g, 5.41 mmol) was added and the reaction mixture was stirred at room temperature for 1.5 h. The reaction was quenched with 50 ml of a 1 :1 solution of 10%> aqueous Na2S203 and saturated aqueous NaHCC>3 and then extracted with dichloromethane (2x). The organic layers were washed with saturated aqueous NaHCC>3, water and brine. The aqueous layers were back extracted with dichloromethane. The organic layers were combined, dried over sodium sulfate, filtered and concentrated. The residue was chromato graphed over silica gel with EtOAc/hexanes (gradient 0-40% EtOAc) to afford 226 mg (45%) of isoxazole-5-carbaldehyde as a colorless oil. 1H NMR (CDC13, 300 MHz): ? (ppm)10.05 (s, 1H), 8.44 (d, J=1.9 Hz, 1H), 7.02 (d, J=1.9 Hz, 1H).

98019-60-4 Isoxazol-5-ylmethanol 12905098, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; CHEN, Shaoqing; DE VICENTE FIDALGO, Javier; HAMILTON, Matthew Michael; HERMANN, Johannes Cornelius; KENNEDY-SMITH, Joshua; LI, Hongju; LOVEY, Allen John; LUCAS, Matthew C.; LUK, Kin-Chun Thomas; LYNCH, Stephen M.; O’YANG, Counde; PADILLA, Fernando; SCHOENFELD, Ryan Craig; SIDDURI, Achyutharao; SOTH, Michael; WANG, Ce; WOVKULICH, Peter Michael; ZHANG, Xiaohu; WO2013/30138; (2013); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem