Month: September 2020

88511-37-9, 1-(Isoxazol-3-yl)ethanone is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

88511-37-9, To a -78 C solution of l-(isoxazol-3-yl)ethanone (2.18 g, 19.62 mmol) in tetrahydrofuran (58 mL) was added lithium hexamethyldisilazide (1 M in toluene, 18 mL, 18 mmol) dropwise over the course of 20 minutes. The solution was warmed to 0 C and stirred for 30 minutes, at which point diethyl oxalate (2.9 mL, 21.6 mmol) was added over the course of 5 minutes. The solution was warmed to room temperature and stirred for 45 minutes. Ethanol (58 mL), hydrazine hydrate (0.88 mL, 18 mmol), and acetic acid (5.8 mL) were sequentially added. The heterogeneous solution was heated to 70 C. After stirring for 2.25 hours at this temperature, the solvent was removed under vacuum. Water (300 mL) and dichloromethane (300 mL) were added, the layers were separated, and the aqueous layer was extracted with dichloromethane (5 x 150 mL). The organics were combined, dried over magnesium sulfate, filtered, and the solvent was removed under vacuum. Purification by silica gel chromatography (0-15% methanol in dichloromethane) and re-purification (ethyl acetate in dichloromethane) gave impure product. The resulting solid was triturated with diethyl ether to give Interraediate-3 (2.21 g, 59%) as a white solid.

As the paragraph descriping shows that 88511-37-9 is playing an increasingly important role.

Reference£º
Patent; IRONWOOD PHARMACEUTICALS, INC.; KIM, Charles; NAKAI, Takashi; MOORE, Joel; PERL, Nicholas, Robert; IM, G-yoon, Jamie; BARDEN, Timothy, Claude; IYENGAR, Rajesh, R.; ZIMMER, Daniel, P.; FRETZEN, Angelika; RENHOWE, Paul, Allan; WO2013/101830; (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.42831-50-5,5-Methylisoxazole-4-carboxylic acid,as a common compound, the synthetic route is as follows.

A round bottomed flask equipped with a mechanical stiner, condenser, thermometer pocket and a stopper were added 5-Methylisoxazole-4-carboxylic acid (3.00 g, 0.02 mol) and Thionyl chloride (14.66 g, 0.12 mol) and the reaction mixture was gradually heated to 45¡À5C and stined at same temperature for 2 to 3 h. The progress of the reaction was monitored by TLC (Acid chloride was analyzed as corresponding methyl ester by quenching the samplein methanol). After the completion of reaction, the reaction mixture was concentrated under reduced pressure at 45¡À5C to afford 5-Methylisoxazole-4-carbonyl chloride as a liquid (0.59 mol).

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; BIOCON LIMITED; PALLE, Venkata, Raghavendracharyulu; BHAT, Ramakrishna, Parameshwar; KALIAPPAN, Mariappan; BABU, Jithendra, R.; SHANMUGHASAMY, Rajmahendra; (39 pag.)WO2016/203410; (2016); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

110256-15-0, 5-Cyclopropylisoxazole-3-carboxylic acid is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

[0267] To a stirred solution of 5-cyclopropylisoxazole-3-carboxylic acid (0.750 g, 4.90 mmol) in DCM (5 ml) was added oxalyl chloride (1.68 ml, 19.60 mmol) and 2 drops of DMF. The reaction was stirred at RT 2 hr. After complete consumption of starting material, the solvent was removed under reduced pressure to obtain 5-cyclopropylisoxazole-3-carbonyl chloride as a residue (0.6 g, crude). The material was used without further purification., 110256-15-0

110256-15-0 5-Cyclopropylisoxazole-3-carboxylic acid 1092113, aIsoxazoles compound, is more and more widely used in various fields.

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
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

Compound 85-a (200.00 mg, 1.77 mmol, 1.00 eq) was dissolved in dichloromethane (15.00 mL), and compound 7-a (305.88 mg, 1.95 mmol, 299.88 mL, 1.10 eq), EDCI (464.54 mg, 2.42 mmol, 1.37 eq), HOBt (327.43 mg, 2.42 mmol, 1.37 eq) and NMM (536.75 mg, 5.31 mmol, 583.42 mL, 3.00 eq) were added thereto. The reaction solution was stirred at 10C for 15 hours. After the reaction was completed, the reaction solution was added with water (100 mL), and extracted with dichloromethane (100 mL 3 3). The organic phases were combined, dried over anhydrous sodium sulfate, filtered and concentrated to give a crude product. The crude product was subjected to column chromatography (petroleum ether : ethyl acetate = 1:0?2:1) to give the product of compound 85-b (380.00 mg, yield: 85%) as a colorless oil. 1H NMR (400 MHz, CHLOROFORM-d) delta=8.31 (d, J=1.51 Hz, 1H), 6.75 (d, J=1.51 Hz, 1H), 4.44 (d, J=13.05 Hz, 1H), 4.14-4.22 (m, 2H), 4.08 (d, J=12.55 Hz, 1H), 3.30 (t, J=11.29 Hz, 1H), 3.10 (t, J=11.04 Hz, 1H), 2.57-2.68 (m, 1H), 1.99 (br. s., 2H), 1.77-1.87 (m, 2H), 1.26-1.29 (m, 3H).

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

Reference£º
Patent; Chia Tai Tianqing Pharmaceutical Group Co., Ltd.; Medshine Discovery Inc.; HE, Haiying; WU, Songliang; LUO, Zhi; MOU, Jianfeng; GUO, Fengying; WANG, Chuan; LI, Guoqing; ZENG, Minggao; CHEN, Shuhui; (199 pag.)EP3456711; (2019); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

32326-25-3, 5-Methoxyisoxazol-3-amine is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

In a reaction flask equipped with a stirrer, a condenser and a thermometer,4.27 g (0.01 mol) of Intermediate IV-2, 2.00 g (0.02 mol) of potassium bicarbonate,30ml of methanol and 1.14g (0.01mol) 5-methoxy-3-aminoisoxazole, the reaction was refluxed 8h,The reaction was complete by TLC, insolubles were filtered off, the solvent was evaporated and the residue was chromatographed on silica gel,Compound I-5 was obtained as a white solid with a yield of 88% and a purity of 99.7% (HPLC normalization method), 32326-25-3

As the paragraph descriping shows that 32326-25-3 is playing an increasingly important role.

Reference£º
Patent; Tianjin Pharmaceutical Institute; Liu Dengke; Liu Ying; Xie Xiaoshuai; Mu Shuai; Zhang Dashuai; Hou Jiajia; Zou Meixiang; (20 pag.)CN103804367; (2016); B;,
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 solution of 5-amino-3-tert-butylisoxazole (0.100 g) in anh toluene (5 mL) was added 4-chloro-3-(trifluoromethyl)phenyl isocyanate (0.395 g). The reaction vessel was sealed, heated at 85 ¡ãC for 24 h, and cooled to room temp. The reaction mixture was added to a slurry of Dowex.(R). 50WX2-100 resin (0.5 g) in CH2Cl2 (40 mL), and the resulting mixture was stirred vigorously for 72 h. The mixture was filtered and the filtrate was concentrated under reduced pressure. The residue was purified by column chromatography (gradient form 100percent CH2Cl2 to 5percent MeOH/95percent CH2Cl2) to give bis(4-chloro-3-(trifluoromethyl)phenyl)urea followed by N-(3-tert-butyl-5-isoxazolyl)-N’-(4-chloro-3-(trifluoromethyl)phenyl)urea. The residue from the symmetrical urea fractions was triturated (Et2O/hexane) to give the urea as a white solid (0.110 g): TLC (3percent MeOH/97percent CH2Cl2) Rf 0.55; FAB-MS m/z 417 ((M+H)+).

59669-59-9 3-(tert-Butyl)isoxazol-5-amine 2095694, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; Bayer Corporation; EP1449834; (2004); A2;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

354795-62-3, 3-Methylisoxazol-4-amine is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

3- ethyl-4-isoxazolamine (38.0 mg, 0.28 mmol), 1-hydroxy-7-azabenzotriazole (30.7 mg, 0.23 mmol), EDC (43.3 mg, 0.23 mmol) and diisopropylethylamine (0.10 ml, 0.56 mmol) were added to a solution of 2-{[(4-fluorophenyl)methyl]oxy}-5-{1-[2-(4- morpholinyl)ethyl]-1 H-pyrazol-4-yl}benzoic acid (may be prepared as described in Description 114; 80 mg, 0.19 mmol) in N,N-dimethylformamide (2 ml) and the reaction mixture was stirred at room temperature overnight. The DMF was removed on a buchi. The residue was taken up into ethyl acetate (50 ml) and washed with water (1 x 25 ml). The ethyl acetate layer was evaporated on a buchi under reduced pressure and the residue was purified using the DAP. The solid obtained after concentrating the appropriate sample was taken up into ethyl acetate (50 ml) and washed with saturated bicarbonate (10 ml). The organic phase was dried (MgS04) and evaporated to yield the title compound as a white solid. 15 mg.MS (electrospray): m/z [M+H]+ = 506H N R (400 MHz, CHLOROFORM-d) delta ppm 1.57 (3 H, s) 2.47 – 2.60 (4 H, m) 2.87 (2 H, t, J=6.65 Hz) 3.66 – 3.79 (4 H, m) 4.29 (2 H, t, J=6.65 Hz) 5.20 (2 H, s) 7.13 – 7.23 (3 H, m) 7.54 (2 H, dd, J=8.53, 5.27 Hz) 7.66 (1 H, dd, J=8.53, 2.26 Hz) 7.79 (2 H, d, J=13.80 Hz) 8.42 (1 H, d, J=2.26 Hz) 9.11 (1 H, s), 354795-62-3

354795-62-3 3-Methylisoxazol-4-amine 13804284, aIsoxazoles compound, is more and more widely used in various fields.

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

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

to a solution of 3-(3-[l-[(tert-butyldimethylsilyl)oxy]ethyl]-l,2,4-oxadiazol-5- yl)cyclobutan-l -amine (1.5 g, 5.04 mmol, 1.00 eq.) in dichloromethane (100 mL)was added 5- phenyl-l,2-oxazole-3-carboxylic acid (1.13 g, 5.97 mmol, 1.20 eq.), HATU (2.28 g, 6.00 mmol, 1.20 eq.) and DIEA (1.93 g, 14.93 mmol, 3.00 eq.). The resulting solution was stirred for 1 hour at room temperature. The reaction was then quenched by the addition of water and extracted with ethyl acetate (3×50 mL) and the combined organic layers were dried over anhydrous sodium sulfate and concentrated under vacuum. The residue was applied onto a silica gel column with ethyl acetate/petroleum ether (l :50)to give 300 mg (13%) of 5-phenyl- N-[cw-3-(3-[l-[(tert-butyldimethylsilyl)oxy]ethyl]-l,2,4-oxadiazol-5-yl)cyclobutyl]-l,2- oxazole-3-carboxamide as a white solid. The solvent was changed to a mixture of with ethyl acetate/petroleum ether (1 :20) to give 1.4 g (59%) of 5-phenyl-N-[fra ,-3-(3-[l-[(tert- butyldimethylsilyl)oxy]ethyl]-l,2,4-oxadiazol-5-yl)cyclobutyl]-l,2-oxazole-3-carboxamide as a white solid. LC-MS: (M+H)+ = 469.

14441-90-8, As the paragraph descriping shows that 14441-90-8 is playing an increasingly important role.

Reference£º
Patent; PROTEOSTASIS THERAPEUTICS, INC.; BASTOS, Cecilia, M.; MUNOZ, Benito; TAIT, Bradley; (178 pag.)WO2016/115090; (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.54593-26-9,3,5-Dimethyl-4-isoxazolecarbaldehyde,as a common compound, the synthetic route is as follows.

54593-26-9, (i) methyl 2-(2-((3,5-dimethylisoxazoi-4-yl)(hydroxy)methyl)benzofuran-Syl)acetate: To a solution of methyl 2?(2-brornoberizofuran-5-yl)acetate (2.0 mg, 7.46 nmmnol) in. 50 niL TI-IF at 0 Cwas added i-PrMgC1 (5.6 mE, 11.2 mniol, 2N in THF). The mixture was stirred at 0 C for 30 mm. Then 3,Sdimethylisoxazole4-carbaldehyde (1.5 g, 12 mmol) was added to the mixture. The resulting mixture was stirred for 2 h. Saturated aq. NHCi (10 mL) was added to the mixture and the mixture was extracted with EtOAc (3 x 50 mL). The combined organic layers were washed with brine (3 x 15 mL) and dried over Na2504. The solvent was evaporated to aresidue which was purified by silica gel column chromatography (30% EtOAc/petroleum ether) to afford the title compound (900 mg, yield 38%) as a yellow oil. LCMS-P1: 316 [M+H] R = i.48i mm.

As the paragraph descriping shows that 54593-26-9 is playing an increasingly important role.

Reference£º
Patent; TEMPERO PHARMACEUTICALS, INC.; BALOGLU, Erkan; GHOSH, Shomir; LOBERA, Mercedes; SCHMIDT, Darby, R.; WO2013/19626; (2013); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

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

a solution of (lS)-l-[5-[(3- aminocyclobutyl)methyl]-l,3,4-thiadiazol-2-yl]ethan-l-ol hydrochloride (1.2 g, 4.80 mmol, 1.00 eq.), 5-phenyl-l,2-oxazole-3-carboxylic acid (2.36 g, 12.48 mmol, 2.60 eq.) and HCTU (6.0 g, 14.50 mmol, 3.00 eq.) in dichloromethane (50 mL) was placed in a 100-mL round- bottom flask. This was followed by the addition of DIEA (3.1 g, 23.99 mmol, 5.00 eq.) dropwise with stirring at 0C. The resulting solution was stirred for 4 hours at room temperature. The reaction was then quenched by the addition of 50 mL of water/ice and extracted with dichloromethane (3×50 mL) and the organic layers combined. The resulting mixture was washed with brine (3×30 mL), dried over anhydrous sodium sulfate and concentrated under vacuum. The residue was applied onto a silica gel column with ethyl acetate/petroleum ether (2: 1). This resulted in 2.1 g (79%) of (lS)-l-(5-[[3-(5-phenyl-l,2- oxazole-3-amido)cyclobutyl]methyl]-l,3,4-thiadiazol-2-yl)ethyl 5-phenyl-l,2-oxazole-3- carboxylate as a off-white solid. LC-MS: (M+H)+ = 556

14441-90-8, The synthetic route of 14441-90-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PROTEOSTASIS THERAPEUTICS, INC.; LEE, Po-shun; (180 pag.)WO2017/40606; (2017); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem