Category: 81282-60-2

Some tips on 81282-60-2

As the paragraph descriping shows that 81282-60-2 is playing an increasingly important role.

81282-60-2, 7-Aminobenzo[d]oxazol-2(3H)-one is a benzoxazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

81282-60-2, Example 1g. Preparation of bifeprunox MESYLATE (crude) 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 10-20C. 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 10C. 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 mi 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 mi 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 rep eated 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 0-5C 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 50C and 100 mbar under a gentle nitrogen stream till dry. Yield about 76%.

As the paragraph descriping shows that 81282-60-2 is playing an increasingly important role.

Reference£º
Patent; SOLVAY PHARMACEUTICALS B.V.; WO2005/16898; (2005); A2;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

Application of trans-Cyclohexane-1,2-diamine

As the rapid development of chemical substances, we look forward to future research findings about 81282-60-2

The benzoxazole compound, name is 7-Aminobenzo[d]oxazol-2(3H)-one,cas is 81282-60-2, mainly used in chemical industry, its synthesis route is as follows.,81282-60-2

To a mixture of 14.9 g N-methyldiethanolamine (3), 44.5 g triethylamine and 120 ml methyl ethyl ketone (MEK) a mixture of 51.6 g methanesulfonic anhydride and 100 ml MEK was dosed at 0 C. Subsequently 14.5 g methanesulfonic acid was dosed at 0 C. After which, 14.5 g 7-amino-2(3H)-benzoxazolone (2) was added and the mixture was heated to reflux followed by a reflux period of 48 hours during which the product crystallized. The product was filtered off after cooling to 0 C. and washed with MEK. The product was dried at 50 C. and 100 mbar to constant weight. The overall yield of this step was about 67% (crude on crude).

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Reference£º
Patent; Rheenen, Jeroen Van; Muijselaar, Wilhelmus G.H.M.; Teunissen, Hendrik; US2011/86862; (2011); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

New learning discoveries about 81282-60-2

The synthetic route of 81282-60-2 has been constantly updated, and we look forward to future research findings.

81282-60-2,81282-60-2, 7-Aminobenzo[d]oxazol-2(3H)-one is a benzoxazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Preparation of 1-(4-(trifluoromethyl)benzyl)-3-(2,3-dihydro-2-oxobenzo[d]oxazol-7-yl)urea Commercially available 4-trifluoromethylbenzylamine (1 ml, 7 mmol) was dissolved in 20 ml of AcOEt and at 0C triphosgene (2 g, 7 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 1c (700 mg, 4.66 mmol) and the mixture was warmed at 80C for 8 hours. (TLC AcOEt 4 / petroleum ether 6). 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 320 mg of a white solid. Yield = 19.5% 1HNMR (DMSO, 400 MHz) delta 4.41 (2H, d, J = 6 Hz), 6.67 (1H, dd, J = 7.6 Hz, J’ = 1.2 Hz), 7.00 (1H, t, J = 8 Hz), 7.09 (1H, t), 7.51 (2H, d, J = 8 Hz), 7.70 (3H, m), 8.73 (1H, s), 10.60 (1H, bs); [M+1] 352.1 (C16H12F3N3O3 requires 351.3).

The synthetic route of 81282-60-2 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

Brief introduction of 81282-60-2

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

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

Simple exploration of 81282-60-2

As the paragraph descriping shows that 81282-60-2 is playing an increasingly important role.

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.

81282-60-2, Step 3 7-(Piperazin-1-yl)benzo[d]oxazol-2(3H)-one: In a 100 mL of round-bottom flask was added a solution of 7-aminobenzo[d]oxazol-2(3H)-one (800 mg, 5.33 mmol), bis-(2-chloro-ethyl)-amine (900 mg, 6.34 mmol), and chlorobenzene (30 ml). The solution was stirred at about 85 C. for about 12 hours. The resulting precipitant was collected by filtration, and washed with ethyl acetate. The filter cake was dried in vacuo to give the title product (0.82 g, yield=70%). LC-MS: m/z=220 (MH)+; H NMR (300 MHz, DMSO) delta 11.67 (s, 1H), 9.34 (s, 1H), 7.04-7.09 (t, J=8.1 Hz, 1H), 6.68-6.73 (t, J=8.1 Hz, 2H), 3.17-3.43 (m, 8H).

As the paragraph descriping shows that 81282-60-2 is playing an increasingly important role.

Reference£º
Patent; AUSPEX PHARMACEUTICALS, INC.; US2010/119622; (2010); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

Introduction of a new synthetic route about 81282-60-2

With the rapid development of chemical substances, we look forward to future research findings about 81282-60-2

7-Aminobenzo[d]oxazol-2(3H)-one, cas is 81282-60-2, it is a common heterocyclic compound, the benzoxazole compound, its synthesis route is as follows.,81282-60-2

Amine 2c (1 g, 3.8 mmol) (Scheme 7) was dissolved in 20 ml of AcOEt and at 0C triphosgene (1.13 g, 3.8 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 lc (390 mg, 2.6 mmol) and the mixture was warmed at 80C for 8 hours. (TLC AcOEt 1 / petroleum ether 1). 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 160 mg of a white solid. Yield = 14% 1HNMR (DMSO, 200 MHz) delta 1.56 (2H, bs), 1.69 (4H, bs), 2.85 (4H, m), 4.42 (2H, d, J = 5.6 Hz), 6.66 (1H, dd, J = 8 Hz, J’ = 0.8 Hz), 7.01 (2H, m), 7.32 (1H, s), 7.44 (2H, dd, J = 7.6 Hz), 7.72 (1H, dd, J = 8.6 Hz, J’ = 1 Hz), 8.73 (1H, bs), 1 1.68 (1H, bs); [M+1] 435.2 (C2iH21F3N4O3 requires 434.4).

With the rapid development of chemical substances, we look forward to future research findings about 81282-60-2

Reference£º
Patent; PHARMESTE S.R.L.; NAPOLETANO, Mauro; TREVISANI, Marcello; PAVANI, Maria Giovanna; FRUTTAROLO, Francesca; WO2011/120604; (2011); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

Introduction of a new synthetic route about 81282-60-2

With the rapid development of chemical substances, we look forward to future research findings about 81282-60-2

7-Aminobenzo[d]oxazol-2(3H)-one, cas is 81282-60-2, it is a common heterocyclic compound, the benzoxazole compound, its synthesis route is as follows.,81282-60-2

Example 35: 1-(4-(trifluoromethyl)-2-(pyrrolidin-1-yl)benzyl)-3-(2,3-dihydro-2-oxobenzo[d]oxazol-7-yl)urea (scheme 1) Preparation of 1-(4-(trifluoromethyl)-2-(pyrrolidin-1-yl)benzyl)-3-(2,3-dihydro-2-oxobenzo[d]oxazol-7-yl)urea Amine 2b (795 mg, 3.3 mmol) was dissolved in 20 ml of AcOEt and at 0C triphosgene (979 mg, 3.3 mmol) was added to the solution. The mixture was warmed at 80C for 4 hours then evaporated and the residue was dissolved in 5ml of DMF. The solution of the isocyanate was added dropwise to a solution in DMF (10 ml) of compound 1c (330 mg, 2.2 mmol) and the mixture was warmed at 80C for 8 hours. (TLC AcOEt 1 / petroleum ether 1). 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 240 mg of a white solid. Yield = 26% 1HNMR (DMSO, 200 MHz) delta 1.91 (4H, m), 3.22 (4H, m), 4.38 (2H, d, J = 5.4 Hz), 6.66 (1H, dd, J = 7.6 Hz, J’ = 1.2 Hz), 7.00 (3H, m), 7.19 (1H, d, J = 8 Hz), 7.39 (1H, d), 7.72 (1H, dd, J = 8.6 Hz, J’ = 1), 8.72 (1H, bs), 11.63 (1H, bs); [M+1] 421.3 (C20H19F3N4O3 requires 420.4).

With the rapid development of chemical substances, we look forward to future research findings about 81282-60-2

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

Analyzing the synthesis route of 81282-60-2

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

81282-60-2, 7-Aminobenzo[d]oxazol-2(3H)-one is a benzoxazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

81282-60-2, Example 35: 1-(4-(trifluoromethyl)-2-(pyrrolidin-1-yl)benzyl)-3-(2,3-dihydro-2-oxobenzo[d]oxazol-7-yl)urea (scheme 1) Preparation of 1-(4-(trifluoromethyl)-2-(pyrrolidin-1-yl)benzyl)-3-(2,3-dihydro-2-oxobenzo[d]oxazol-7-yl)urea Amine 2b (795 mg, 3.3 mmol) was dissolved in 20 ml of AcOEt and at 0C triphosgene (979 mg, 3.3 mmol) was added to the solution. The mixture was warmed at 80C for 4 hours then evaporated and the residue was dissolved in 5ml of DMF. The solution of the isocyanate was added dropwise to a solution in DMF (10 ml) of compound 1c (330 mg, 2.2 mmol) and the mixture was warmed at 80C for 8 hours. (TLC AcOEt 1 / petroleum ether 1). 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 240 mg of a white solid. Yield = 26% 1HNMR (DMSO, 200 MHz) delta 1.91 (4H, m), 3.22 (4H, m), 4.38 (2H, d, J = 5.4 Hz), 6.66 (1H, dd, J = 7.6 Hz, J’ = 1.2 Hz), 7.00 (3H, m), 7.19 (1H, d, J = 8 Hz), 7.39 (1H, d), 7.72 (1H, dd, J = 8.6 Hz, J’ = 1), 8.72 (1H, bs), 11.63 (1H, bs); [M+1] 421.3 (C20H19F3N4O3 requires 420.4).

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

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

New learning discoveries about 81282-60-2

The synthetic route of 81282-60-2 has been constantly updated, and we look forward to future research findings.

81282-60-2, 7-Aminobenzo[d]oxazol-2(3H)-one is a benzoxazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 36: 1-(4-(trifluoromethyl)-2-(piperidin-1-yl)benzyl)-3-(2,3-dihydro-2-oxobenzo[d]oxazol-7-yl)urea (scheme 1) Preparation of 1-(4-(trifluoromethyl)-2-(piperidin-1-yl)benzyl)-3-(2,3-dihydro-2-oxobenzo[d]oxazol-7-yl)urea Amine 2c (1 g, 3.8 mmol) was dissolved in 20 ml of AcOEt and at 0C triphosgene (1.13 g, 3.8 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 1c (390 mg, 2.6 mmol) and the mixture was warmed at 80C for 8 hours. (TLC AcOEt1 / petroleum ether 1). 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 160 mg of a white solid. Yield = 14% 1HNMR (DMSO, 200 MHz) delta 1.56 (2H, bs), 1.69 (4H, bs), 2.85 (4H, m), 4.42 (2H, d, J = 5.6 Hz), 6.66 (1H, dd, J = 8 Hz, J’ = 0.8 Hz), 7.01 (2H, m), 7.32 (1H, s), 7.44 (2H, dd, J = 7.6 Hz), 7.72 (1H, dd, J = 8.6 Hz, J’ = 1 Hz), 8.73 (1H, bs), 11.68 (1H, bs); [M+1] 435.2 (C21H21F3N4O3 requires 434.4).

The synthetic route of 81282-60-2 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

Simple exploration of 81282-60-2

As the paragraph descriping shows that 81282-60-2 is playing an increasingly important role.

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.

Commercially available 4-trifluoromethylbenzylamine (1 ml, 7 mmol) was dissolved in 20 ml of AcOEt and at 0C triphosgene (2 g, 7 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 lc (700 mg, 4.66 mmol) and the mixture was warmed at 80C for 8 hours. (TLC AcOEt 4 / petroleum ether 6). 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 320 mg of a white solid. Yield = 19.5% ‘HNMR (DMSO, 400 MHz) delta 4.41 (2H, d, J = 6 Hz), 6.67 (1H, dd, J = 7.6 Hz, J’ = 1.2 Hz), 7.00 (1H, t, J = 8 Hz), 7.09 (1H, t), 7.51 (2H, d, J = 8 Hz), 7.70 (3H, m), 8.73 (1H, s), 10.60 (1H, bs); [M+1] 352.1 (C16H12F3N3O3 requires 351.3).

As the paragraph descriping shows that 81282-60-2 is playing an increasingly important role.

Reference£º
Patent; PHARMESTE S.R.L.; NAPOLETANO, Mauro; TREVISANI, Marcello; PAVANI, Maria Giovanna; FRUTTAROLO, Francesca; WO2011/120604; (2011); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem