Month: September 2020

81900-93-8, 4-Aminobenzo[d]oxazol-2(3H)-one is a benzoxazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

81900-93-8, Example 29: 1-(2-(dimethylamino)-4-(trifluoromethyl)benzyl)-3-(2,3-dihydro-2-oxobenzo[d]oxazol-4-yl)urea scheme 1) Preparation of 1-(2-(dimethylamino)-4-(trifluoromethyl)benzyl)-3-(2,3-dihydro-2-oxobenzo[d]oxazol-4-yl)urea Amine 2a (1.2 g, 5.5 mmol) was dissolved in 40ml of AcOEt and at 0C triphosgene (1.63 g, 5.5 mmol) was added to the solution. The mixture was warmed at 80C for 4 hours then evaporated and the residue was dissolved in 5 ml of DMF. The solution of the isocyanate was added dropwise to a solution in DMF (10 ml) of compound 1b (820 mg, 5.5 mmol) and the mixture was warmed at 80C for 8 hours. (TLC AcOEt 7 / petroleum ether 3). The solvent was evaporated and the crude was dissolved in AcOEt (50 ml) and washed with water (1 X 3 0ml) and brine. The organic phase was dried over sodium sulfate and concentrated under vacuum. The purification of the crude residue by chromatographic column gave 300 mg of a white solid. Yield = 14% 1HNMR (DMSO, 200 MHz) delta 2.51 (6H, s), 4.71 (2H, d, J = 5.6 Hz), 6.55 (2H, d, J = 8.2 Hz), 7.05 (1H, t, J = 7.6 Hz), 7.40 (1H, m), 7.51 (1H, d), 10.06 (1H, bt), 11.53 (1H, bs), 11.80 (1H, bs); [M+1] 395.1 (C18H17F3N4O3 requires 394.35).

As the paragraph descriping shows that 81900-93-8 is playing an increasingly important role.

Reference£º
Patent; Pharmeste S.r.l.; EP2377850; (2011); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

81282-60-2,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.81282-60-2,7-Aminobenzo[d]oxazol-2(3H)-one,as a common compound, the synthetic route is as follows.

A solution of 128.9 g of 3-[[bis(2-hydroxyethyl)amino]methyl]-1,1′-biphenyl in approximately 750 ml of methylethylketone prepared according to Example 1f was stirred under mild nitrogen purge. In a separate vessel 202 g of methanesulfonic anhydride was dissolved in in 600 ml of methylethylketone at 10-20 C. To the solution of 3-[[bis(2-hydroxyethyl)amino]methyl]-1,1′-biphenyl in methylethylketone 212.8 g of triethylamine was added and 60 ml of methylethylketone. The solution of methanesulfonic anhydride was added in about 45-60 minutes to the 3-[[bis(2-hydroxyethyl)amino]methyl]-1,1′-biphenyl/triethylamine solution, while maintaining the temperature below 10 C. 60 ml of methylethylketone was added and the mixture was stirred for another 15 minutes, followed by drop wise addition of 109.7 g of methanesulfonic acid and addition of 60 ml of methylethylketone in order to rinse the addition vessel. 71.3 g of 7-amino-2(3H)-benzoxazolone, prepared according to Example 1e was suspended in 100 ml of methylethylketone and added to the reaction mixture followed by 60 ml of methylethylketone. The reaction mixture was heated to reflux and refluxed during 20-24 hours. After 20-24 hours of reflux 48 ml of water was added and the mixture was refluxed again for 1 hour. 420 ml of methylethylketone was added and 490 ml of methylethylketone/water was distilled of. This last step was repeated three times. 46.1 g of methanesulphonic acid was added, the mixture was refluxed for an additional hour and cooled down to room temperature in 1 hour. The mixture was further cooled down to 0-5 C. and stirred at this temperature for another hour. The solid was filtered off and, washed twice with 75 ml of cold methylethylketone, and dried at 50 C. and 100 mbar under a gentle nitrogen stream till dry. Yield about 76%.

81282-60-2 7-Aminobenzo[d]oxazol-2(3H)-one 11147814, abenzoxazole compound, is more and more widely used in various fields.

Reference£º
Patent; Eijgendaal, Irene; Klein, Gerrit; Terhorst-Van Amstel, Maria J.L.; Zwier, Klaas; Bruins, Nico; Rigter, Hendrikus T.; Gout, Erik; US2006/40932; (2006); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

81900-93-8,81900-93-8, 4-Aminobenzo[d]oxazol-2(3H)-one is a benzoxazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 26: 1-(2-chloro-4-(trifluoromethyl)benzyl)-3-(2,3-dihydro-2-oxobenzo[d]oxazol-4-yl)urea (scheme 1) Preparation of 1-(2-chloro-4-(trifluoromethyl)benzyl)-3-(2,3-dihydro-2-oxobenzo[d]oxazol-4-yl)urea Commercially available 2-chloro-4-trifluoromethylbenzylamine (572 mg, 2.7 mmol) was dissolved in 20ml of AcOEt and at 0C triphosgene (809 mg, 2.7 mmol) was added to the solution. The mixture was warmed at 80C for 4 hours then evaporated and dissolved in 5 ml of DMF. The solution of the isocyanate was added dropwise to a solution in DMF (5 ml) of compound 1b (270 mg, 1.8 mmol) and the mixture was warmed at 80C for 8 hours. (TLC AcOEt). The solvent was evaporated and the crude was dissolved in AcOEt (30 ml) and washed with water (1 X 20 ml) and brine. The organic phase was dried over sodium sulfate and concentrated under vacuum. The purification of the crude residue by chromatographic column gave 70 mg of a white solid. Yield = 10% 1HNMR (DMSO, 400 MHz) delta 4.45 (2H, d, J = 6 Hz), 6.97 (2H, d, J = 4.4 Hz), 7.07 (2H, m), 7.63 (1H, d, J = 8 Hz), 7.74 (2H, d), 7.86 (1H, s), 8.61 (1H, bs), 10.90 (1H, bs); [M+1] 386.6 (C16H11ClF3N3O3 requires 385.7).

The synthetic route of 81900-93-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Pharmeste S.r.l.; EP2377850; (2011); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

5676-60-8, 2-Methylbenzo[d]oxazol-6-amine is a benzoxazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5676-60-8

EXAMPLE 29- PREPARATION OF N-(2-METHYL-1,3-BENZODIOXOL-6-YL)-2,4- DIMETHYLIMIDAZO[1,5-a]PYRIMIDINE-8-CARBOXAMIDE To a stirred solution of 2,4-dimethylimidazo[1,5-a]pyrimidine-8-carboxylic acid 3 (50 mg, 0.262 mmol), 2-methyl-1,3-benzoxazol-6-amine (47 mg, 0.314 mmol) and HATU (149 g, 0.393 mmol) in DMF (1 mL) was added DIPEA (0.1 mL, 0.524 mmol), and the reaction mixture was stirred at room temperature for 16 hours until the reaction was complete. The suspension was diluted with H2O (3 mL), and the precipitated solid was collected by filtration, washed with minimum DCM and Et2O, and dried in vacuo to give the title compound (57 mg, 68%) as a white solid.1H NMR (400 MHz, DMSO-d6) delta 10.39 (s, 1H), 8.48 (s, 1H), 8.36 (s, 1H), 7.60 (s, 2H), 6.90 (d, J = 1.2 Hz, 1H), 2.71 (s, 3H), 2.61 (s, 3H), 2.60 (s, 3H). ES-MS m/z: 322.0 [M+H]+. HPLC Purity (214 nm): >98%; tR = 8.17 min.

The synthetic route of 5676-60-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; LYSOSOMAL THERAPEUTICS INC.; SKERLJ, Renato, T.; LANSBURY, Peter, T.; GOOD, Andrew, C.; BOURQUE, Elyse Marie, Josee; (134 pag.)WO2016/73889; (2016); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.128156-54-7,Methyl benzo[d]oxazole-4-carboxylate,as a common compound, the synthetic route is as follows.

General procedure: To a degassed solution (N2 was purged for 10 min) of methyl 1,3-benzoxazole-4-carboxylate (150 mg, 0.847mmol) and N-(2-iodophenyl)benzamide 2a (273 mg, 0.847 mmol) in anhydrous toluene (4ml) , CuI (32 mg, 0.169 mmol), xantphos (98 mg, 0.169 mmol), Pd(OAc)2 (10 mg, 0.042 mmol), Cs2CO3 (685 mg, 2.117 mmol) were added at room temperature under nitrogen atmosphere. Reaction mixture was continued for 20 hours at reflux condition. After the completetion of the reaction (monitored by TLC), Reaction mixture was filtered through celite bed and washed with methanol (10 ml),filtrate was concentrated. Crude mass which was purified by column chromatography over silica gel (230-400 mesh) using DCM-Methanol (1:9) as elutant to affordthe products 3a (284 mg) as white solid. All the other compounds 3b-3r were prepared similarly following the above procedure., 128156-54-7

As the paragraph descriping shows that 128156-54-7 is playing an increasingly important role.

Reference£º
Article; Sasmal, Swarnendu; Sen, Indira; Hall, Roger G.; Pal, Sitaram; Tetrahedron Letters; vol. 56; 11; (2015); p. 1374 – 1377;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

81900-93-8, 4-Aminobenzo[d]oxazol-2(3H)-one is a benzoxazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,81900-93-8

Example 32: 1-(4-(trifluoromethyl)-2-morpholinobenzyl)-3-(2,3-dihydro-2-oxobenzo[d]oxazol-4-yl)urea (scheme 1) Preparation of 1-(4-(trifluoromethyl)-2-morpholinobenzyl)-3-(2,3-dihydro-2-oxobenzo[d]oxazol-4-yl)urea Amine 2d (362 mg, 3.8 mmol) was dissolved in 20 ml of AcOEt and at 0C triphosgene (1.12 g, 1equiv.) was added to the solution. The mixture was warmed at 80C for 4 hours then evaporated and the residue was dissolved in 5 ml of DMF. The solution of the isocyanate was added dropwise to a solution in DMF (10 ml) of compound 1b (384 mg, 2.56 mmol) and the mixture was warmed at 80C for 8 hours. (TLC AcOEt). The solvent was evaporated and the crude was dissolved in AcOEt (30 ml) and washed with water (1 X 20 ml) and brine. The organic phase was dried over sodium sulfate and concentrated under vacuum. The purification of the crude residue by chromatographic column gave 200 mg of a pale rose solid. Yield = 18% 1HNMR (DMSO, 400 MHz) delta 2.91 (4H, m), 3.76 (4H, m), 4.46 (2H, d, J = 5.6 Hz), 6.97 (3H, m), 7.05 (1H, m), 7.36 (1H, s), 7.46 (1H, d), 7.54 (1H, d), 8.53 (1H, s), 11.00 (1H, bs); [M+1] 437.1 (C20H19F3N4O4 requires 436.4).).

As the paragraph descriping shows that 81900-93-8 is playing an increasingly important role.

Reference£º
Patent; Pharmeste S.r.l.; EP2377850; (2011); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

701-16-6,701-16-6, 5-Fluoro-2-methylbenzo[d]oxazole is a benzoxazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: The SBOs were prepared by the base-catalysed condensation of the appropriate 5-halogeno-2-methylbenzoxazole with the requisite aromatic aldehyde under phase transfer conditions. In a typical experiment, equimolar quantities (5 mmol) of the starting materials were dissolved in dichloromethane (20-50 ml) in the presence of benzyltriethylammonium chloride (3 mmol) and stirred magnetically under a nitrogen atmosphere as an aqueous solution of sodium hydroxide (50%, w/v, 5 ml) was added dropwise over a period of 10 min. After being stirred for 2-36 h until analytical thin layer chromatography indicated that the reaction was complete, the mixture was diluted with water (50 ml) and the SBO was extracted with dichloromethane (3¡Á20 ml), dried (MgSO4), filtered, evaporated under reduced pressure and recrystallized from aqueous methanol or ethanol.

701-16-6 5-Fluoro-2-methylbenzo[d]oxazole 2769350, abenzoxazole compound, is more and more widely used in various fields.

Reference£º
Article; Ayrton, Stephen T.; Panova, Jekaterina; Michalik, Adam R.; Martin, William H.C.; Gallagher, Richard T.; Bowen, Richard D.; International Journal of Mass Spectrometry; vol. 345-347; (2013); p. 120 – 131;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.22876-19-3,5-Chlorobenzo[d]oxazole-2(3H)-thione,as a common compound, the synthetic route is as follows.

Thionyl chloride (885 g, 7.5 mol)And N, N-dimethylformamide (270 ml) were added to a solution of 5-chloro-2-mercaptobenzoxazole (540 g, 2.903 mol) in dichloromethane (5 L) at 5-10 C.Stirred until a clear solution was formed and the reaction solution was stirred at room temperature for 4 hours.After completion of the reaction, the reaction solution was poured into 4 L of ice water, neutralized to neutral with sodium bicarbonate in 1 hour, and extracted with dichloromethane (2.5 L * 2).The organic layer was washed with brine, dried over sodium sulfate and dried to give the crude product. The crude product was washed with n-hexane (2 L * 2) at -20 C, filtered and dried to give yellow liquid 2,5-dichlorobenzo (496.8 g, 91.0%).

22876-19-3, 22876-19-3 5-Chlorobenzo[d]oxazole-2(3H)-thione 708870, abenzoxazole compound, is more and more widely used in various fields.

Reference£º
Patent; Shanghai ZaiQi Bio-Tech Co., Ltd.; Wang, Zhiguo; Song, Yanhong; Ma, Xiujuan; Tian, Beibei; Li, Shijiang; Li, Chao; Li, Qiang; Li, Tao; (8 pag.)CN106478537; (2017); A;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.924869-17-0,Methyl benzo[d]oxazole-5-carboxylate,as a common compound, the synthetic route is as follows.,924869-17-0

General procedure: To an oven dried 25 mL round bottom flask, palladium complex (7 mg, 3 mol %), cesium carbonate (325 mg, 1 mmol), silver(I) oxide (229 mg, 1 mmol) and azole substrate (0.5 mmol) in 2 mL DMF, under air, were added. Phenyl acetylene substrate (1 mmol) in DMF (2 mL) was added to the reaction vessel slowly by dropping funnel over 2 h while stirring the reaction mixture on preheated oil bath at 85 C. The reaction was allowed to stir for 6 h at the same temperature. The reaction mixture was diluted with EtOAc then filtered through filter paper. The filtrate was quenched with Ice coldwater and then, aqueous layer was extracted with EtOAc. The organic phase was washed with NaCl (satd aq), dried over Na2SO4, and concentrated under reduced pressure. The residue was purified by silica gel column chromatography.

As the paragraph descriping shows that 924869-17-0 is playing an increasingly important role.

Reference£º
Article; Parsharamulu, Thupakula; Vishnuvardhan Reddy, Police; Likhar, Pravin R.; Lakshmi Kantam, Mannepalli; Tetrahedron; vol. 71; 13; (2015); p. 1975 – 1981;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

4570-41-6, Benzo[d]oxazol-2-amine is a benzoxazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 1 ethyl 6-hydroxy-4-oxo-1,2-dihydro-4H-pyrrolo [3,2,1-ij] quinoline-5-carboxylate (130 mg, 0.50 mmol) and benzo[d]oxazol-2-amine (80 mg, 0.60 mmol) is dissolved in DMF (2 mL) and placed in a sealed tube, heated at 160C for 30 minutes, Cooled slowly to room temperature. The resulting solid was filtered and washed with ethanol to give the target compound (KCNS-SM-31); 73 mg, 42% yield).

4570-41-6, 4570-41-6 Benzo[d]oxazol-2-amine 20707, abenzoxazole compound, is more and more widely used in various fields.

Reference£º
Patent; Korea Research Institute of Chemical Technology; Park Cheol-min; Lee Seon-gyeong; Song Jong-hwan; (39 pag.)KR2019/67546; (2019); A;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem