Day: November 9, 2020

1750-42-1, Isoxazol-3-amine is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Intermediate 10: 3-Amino-4-chloroisooxazole.; To a 50 ml_ round-bottomed flask were added a stirbar, 506 mg (6.01 mmol) 3-aminoisoxazole, 15 ml_ DMF and 1.04 g (7.75 mmol) N-chlorosuccinimide. The flask was purged with nitrogen and heated at 50 0C for 48 h. The reaction mixture was then concentrated to dryness in vacuo, the residue taken up in DCM and washed with 1 N NaOH containing Na2S2O3. The organic layer was dried over MgSO4, filtered and evaporated to dryness to give a brown oil. Subjecting the residue to FCC (0-5% 2 N NH3 in MeOH/DCM) gave the pure product as a pale- yellow solid (335.4 mg, 47%). MS (ESI+): Calcd for C3H3N2OCI [M+H]+, m/z 117.99, found 119.0 (M + H)+. 1H NMR (500 MHz, CDCI3): 8.10 (s, 1 H), 4.26 (br s, 2H)., 1750-42-1

The synthetic route of 1750-42-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; JANSSEN PHARMACEUTICA NV; BREITENBUCHER, J., Guy; KEITH, John, M.; TICHENOR, Mark, S.; CHAMBERS, Alison, L.; JONES, William, M.; HAWRYLUK, Natalie, A.; TIMMONS, Amy, K.; MERIT, Jeffrey, E.; SEIERSTAD, Mark, J.; WO2010/68453; (2010); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

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

Preparation of compound A6e: [Show Image] To the solution of benzotrizole (17.85 g, 194.3 mmol) in 100 mL of dry DCM was added SOCl2 (23.09 g, 73.7 mmol) at 0C, and stirred at room temperature for 1 hour. The resulting mixture was added to the solution of compound A5e (55 g, 194.3 mmol) in 500 mL of dry DCM at room temperature and stirred for 1.5 h. 120 mL of water was added to the mixture for quench, and the mixture was extracted with DCM. The organic layer was washed with 1 N aq. NaOH solution, dried over Na2SO4, filtered, concentrated and purified by chromatography on silica gel (eluent: PE/EtOAc = 10/1) to give 47.4 g of compound A6e as a white solid (Yield: 81 %). 1H NMR (400 MHz, CDCl3): delta 1.23-1.33 (m, 4H), 2.14 (m, 1H), 4.40 (s, 2H), 8.31 (s, 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; EP2289883; (2011); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

14678-02-5, 5-Amino-3-methylisoxazole is a Isoxazoles compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

3-Methylisoxazol-5-amine (2.9 g) and potassium carbonate (9.8 g) were suspended in dichloromethane (100 mL) at room temperature 2-bromoacetyl bromide (6 g) was added dropwise. The mixture was allowed to stir overnight. Water (0.3 mL) was added together with a further quantity of potassium carbonate (3 g) and the reaction stirred for a further 30 minutes. The reaction mixture was poured into water (100 mL) and extracted with dichloromethane (2 x 50 mL). The combined organic extracts were dried over Magnesium Sulfate and then evaporated in vacuo. The crude product was purifed by column chromatography on silica eluting with ethyl actetate / isohsxane (50:50) to give sub-titled compound (4.8 g).1H NMR (299.946 MHz, CDCl3) delta 11.97 (s, IH)5 6.16 (s, IH), 4.09 (s, 2H), 2.19 (s, 3H).

14678-02-5, The synthetic route of 14678-02-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2008/59245; (2008); 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.25742-00-1,(3-Bromoisoxazol-5-yl)methanol,as a common compound, the synthetic route is as follows.

To a chilled (O0C) solution of 3-bromo-isoxazol-5-yl)-methanol (560 mg, 3.15 mmol) in CH2Cl2 (31 niL) was added Dess-Martin periodinane (2.00 g, 4.72 mmol) in 3 portions and the mixture was warmed to room temperature. After 4 hours, the mixture was diluted with Et2O (40 mL) and 1:1 mixture of aqueous solution of saturated aqueous NaHCO3 (20 mL) and saturated aqueous Na2S2O3 (20 mL) was added. After 15 hours, the aqueous layer was separated and extracted with Et2O (2 x) and EtOAc (2 x). The combined organic layers were washed with brine, dried over Na2SO4, filtered and concentrated in vacuo to afford S-bromo-isoxazole-S-carbaldehyde as a yellowish/orange solid. MS m/z 194.00 (M+ H2O); 195.97 (M+2).

25742-00-1, 25742-00-1 (3-Bromoisoxazol-5-yl)methanol 2763220, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; COOK, Brian Nicholas; DISALVO, Darren; FANDRICK, Daniel Robert; HARCKEN, Christian; KUZMICH, Daniel; LEE, Thomas Wai-Ho; LIU, Pingrong; LORD, John; MAO, Can; NEU, Jochen; RAUDENBUSH, Brian Christopher; RAZAVI, Hossein; REEVES, Jonathan Timothy; SONG, Jinhua, J.; SWINAMER, Alan, David; TAN, Zhulin; WO2010/36632; (2010); 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.5765-44-6,5-Methylisoxazole,as a common compound, the synthetic route is as follows.

5765-44-6, Example 11A Sodium 1-cyanoprop-1-en-2-olate Sodium (7.69 g, 335 mmol) is introduced in portions into 350 ml of anhydrous methanol. After the reaction mixture has been cooled to 25 C., 5-methylisoxazole (27.8 g, 335 mmol) is slowly added in portions (exothermic reaction). After the addition is complete, the mixture is stirred at RT for 4 h and then concentrated. The residue is washed with a little diethyl ether, filtered off with suction and dried under oil pump vacuum. 32.0 g (91% of theory) of the title compound are obtained. 1H-NMR (400 MHz, DMSO-d6): delta=3.18 (s, 1H), 1.51 (s, 3H).

5765-44-6 5-Methylisoxazole 79833, aIsoxazoles compound, is more and more widely used in various fields.

Reference£º
Patent; BAYER SCHERING PHARMA AKTIENGESELLSCHAFT; US2010/305052; (2010); 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.3405-77-4,5-Methylisoxazole-3-carboxylic acid,as a common compound, the synthetic route is as follows.

(2R,6S,13aS,14aR,16aS,Z)-ethyl 6-(5-methylisoxazole-3-carboxamido)-2-(4- nitrobenzoyloxy)-5,16-dioxo-l,2,3,5,6,7,8,9,10,l l,13a,14,14a,15, 16,16a- hexadecahydrocyclopropa[e]pyrrolo[l,2-a][l,4]diazacyclopentadecine-14a-carboxylate; To a solution of (2R,6S,13aS,14aR,16aS,Z)-14a-(ethoxycarbonyl)-2-(4-nitrobenzoyloxy)- 5,16-dioxo-l,2,3,5,6,7,8,9,10,l l,13a,14,14a,15,16,16a- hexadecahydrocyclopropa[e]pyrrolo[l,2-a][l,4]diazacyclopentadecin-6-aminium 4- methylbenzenesulfonate (9.95 g), 5-methylisoxazole-3-carboxylic acid (2.12 g), and NMP (30.0 g) at 5 ¡ãC was added diisopropylethylamine (6.5 g). Propanephosphonic acid anhydride (5.3 g) was charged as a solution in EtOAc (5.3 g) and NMP (10 mL) to the reaction mixture. The reaction was warmed to rt over 14 h. The reaction solution was diluted with 2-Me-THF (150 mL). The diluted reaction solution was washed with water (150 mL), a 1.0 M aqueous solution of H3PO4 (2 x 50 mL), water (50 mL), a 5percent aqueous solution of NaHC03 (50 mL), and then a 10percent aqueous solution of NaCl (2 x 50 mL). The organic solution was dried over MgS04, filtered, and then concentrated under reduced pressure, and then co-distilled with THF (200 mL). THF was added and the product-containing solution was filtered and evaporated to an oil (8.5 g, 93percent yield).

3405-77-4, The synthetic route of 3405-77-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ABBOTT LABORATORIES; ENANTA PHARMACEUTICALS, INC.; CHEN, Hui-ju; MCDANIEL, Keith, F.; GREEN, Brian, E.; SHANLEY, Jason, P.; KRUGER, Albert, W.; GANDARILLA, Jorge; WELCH, Dennie, S.; CINK, Russell, D.; GAI, Yonghua; WANG, Guoqiang; OR, Yat, Sun; WO2011/156337; (2011); A2;,
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

To a solution of 5-methylisoxazole-3-carboxylic acid (284.0 mg, 2236.0 mumol) dissolved in DCM(lO.OmL) was added HATU (1020.0 mg, 2683.0 mumol) followed by DIEA(586mul, 3353 mumol). The solution was stirred at room temperature for 5 minutes. 4-amino-2-(l- methyl-lH-pyrazol-5-yl)phenol (500.00 mg, 2236 mumol) was added and the reaction mixture was stirred at 25¡ãC for 15 hours. The reaction mixture was subjected to purification by column chromatography (ethyl acetate rhexane 50:50) to afford the title compound as an off- white solid in 59.0percent yield. LCMS m/z = 333.2 (M+H), 1H NMR (400 MHz5 OMSO-d) delta ppm 2.69 (s, 3H), 3.66 (s, 3 H), 6.64 (s, 1 H), 7.00 (d, /=8.84 Hz, 1 H), 7.61 (s, 1 H), 7.64 (d, /=2.53 Hz, 1 H), 7.73 (dd, /=8.84, 2.53 Hz, 1 H), 10.04 (s, 1 H), 10.60 (s, 1 H).

3405-77-4, The synthetic route of 3405-77-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ARENA PHARMACEUTICALS, INC.; WO2007/136703; (2007); 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.21169-71-1,Isoxazole-5-carboxylic acid,as a common compound, the synthetic route is as follows.

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

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;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.14678-02-5,5-Amino-3-methylisoxazole,as a common compound, the synthetic route is as follows.

General procedure: A solution of 2-(chloroseleno)benzoyl chloride (1 mmol) in dryether (10 mL) was added dropwise over 30 min to a stirred solution ofthe appropriate amine (1.2 mmol) and triethylamine (3.5 mmol) in dryDCM (10 mL) at 0 C. The reaction mixture was stirred at room temperatureovernight. The solvent was removed under reduced pressureand the residue was washed with water (20 mL), and extracted withDCM (3¡Á10 mL). The combined organic extracts were dried over anhydrousMgSO4, the solvent removed was under reduced pressure, andthe crude product was purified by flash column chromatography onsilica gel (eluents: 10-50% ethyl acetate in petroleum gradient) [31].All EB analogues except 4c and 4e have been reported., 14678-02-5

The synthetic route of 14678-02-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Chen, Cheng; Yang, Kewu; Bioorganic Chemistry; vol. 93; (2019);,
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

To a mixture of 5-cyclopropylisoxazole-3-carboxylic acid (50 mg, 0.32 mmol) in DMF (1 mL) was added HATU (120 mg, 0.32 mmol) under N2, the mixture was stirred for 30 mm, then c/s-i[5 -[3 -(trifluoromethoxy)cyclobutylj -1,3 ,4-oxadiazol-2-yl Ibicyclo [1.1.1 jpentan-3 -amine hydrochloride (8:1 to 10:1 favoring the cis- diastereomer) (89 mg, 0.27 mmol) and DIEA (140 mg, 1.1 mmol) were added to the solution at 0 C. The reaction mixture was stirred at 20 C for 12 h. The reaction mixture was quenched by addition of H20 (10 mL) at 0 C and extracted with EtOAc (3 x 10 mL). The combined organic layers were washed with brine (10 mL), dried over anhydrous Na2SO4, filtered, and concentrated under reduced pressure. The cmde reaction mixture was purified employing reverse- phase HPLC. LC-MS, mlz = 425.3 [M+Hfb. ?H-NMR (400 MHz, CDC13): 7.25 (s, 1H), 6.32 (s, 1H), 4.71 (quin, J= 7.56 Hz, 1H), 3.40-3.26 (m, 1H), 2.94-2.81 (m, 2H), 2.74-2.69 (m, 2H), 2.686H), 2.15-2.03 (m, 1H), 1.19-1.08 (m, 2H), 1.03-0.94 (m, 2H).

110256-15-0, As the paragraph descriping shows that 110256-15-0 is playing an increasingly important role.

Reference£º
Patent; DENALI THERAPEUTICS INC.; CRAIG, Robert A., II; ESTRADA, Anthony A.; FENG, Jianwen A.; FOX, Brian; HALE, Christopher R. H.; LEXA, Katrina W.; OSIPOV, Maksim; REMARCHUCK, Travis; SWEENEY, Zachary K.; DE VICENTE FIDALGO, Javier; (187 pag.)WO2019/32743; (2019); A1;,
Isoxazole – Wikipedia
Isoxazole | C3H3NO – PubChem