Tag: 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.

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

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

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

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

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

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

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

To a solution of [6-(trifluoromethyl)-3-pyridyl)]-methanamine (lg, 4.7 mmol) in THF (30 mL) was added CDI (2.1 mol eq) and the mixture was heated at 70C overnight. The reaction mixture was evaporated, water was added and the aqueous phase was extracted with EtOAc (3×20 mL). The recombined organic phases were anhydrified over Na2SO4 and evaporated at reduced pressure (quantitative yield). The oil obtained (0.34g, 1.2 mmol) was dissolved in DMF (15 mL) and the bicyclic amine lc (Scheme 3) was added (0.8 mol eq), then the mixture obtained was heated at 100C overnight. The solvent was removed at reduced pressure and the residue was purified by chromatography (1 : 1 EtOAc:petroleum ether) to obtain the product as a white solid (0.064g, 20% Yield). ‘HNMR (DMSO, 200 MHz) delta 4.46 (d, 2H, J=6), 6.66 (d, 1H, J=8), 6.96 (t, 1H), 7.04 (bt, 1H), 7.64 (d, 1H, J=8), 7.86 (m, 2H), 8.70 (s, 1H), 8.77 (s, 1H), 1 1.60 (bs, 1H). [M+1] 358.02 (Ci5HnF3N4O3 requires 357.27).

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

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.

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).

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

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.

4-trifluoromethylphenylacetic acid (453 mg, 2.2 mmol) was dissolved in 20 ml of THF and at 0C DEPC (0.43 ml, 1.3equiv) and amine lc (400 mg, 2.66 mmol) were added to the solution. The mixture was warmed at 80C overnight, then 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 using AcOEt 3 /petroleum ether 7 as eluant gave 340 mg of a white solid. Yield = 46% 1HNMR (DMSO, 200 MHz) delta 3.86 (2H, s), 6.86 (1H, d), 7.06 (1H, t), 7.58 (3H, m), 7.70 (2H, d, J = 8.4 Hz), 10.32 (1H, bs), 8.73 (1H, bs), 1 1.80 (1H, bs); [M+1] 337.2 (C 16H11F3N2O3 requires 336.3).

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.; NAPOLETANO, Mauro; TREVISANI, Marcello; PAVANI, Maria Giovanna; FRUTTAROLO, Francesca; WO2011/120604; (2011); 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.81282-60-2,7-Aminobenzo[d]oxazol-2(3H)-one,as a common compound, the synthetic route is as follows.

4.91 g (32.7 mmol) of the anilin was suspended in 75 ml of 48% of HBr/water, while it was cooled to -5 C. Subsequently 2.27 g (33 mmol) of sodium nitrite dissolved in 4 ml of water, were added dropwise during 15 minutes. Stirring was continued at 0 C. for 15 minutes. Subsequently, the reaction mixture was added, in one time, to a 0 C. solution of 2.42 g (16.9 mmol) CuBr in 20 ml of 48% HBr/water. After 30 minutes the reaction mixture was heated to 85 C. for one hour, after which it was allowed to reach room temperature, stirring was continued for 14 hours. To the mixture diethyl ether and water were added, after shaking the organic layer was isolated which was washed with water. The organic layer, together with some silica, was concentrated in vacuo, and the residue was put on top of a flash chromatography column (SiO2) using Et2O/petroleum ether (1/1), and later on pure Et2O as the eluent. The combined product containing fractions yielded after concentration in vacuo 3.3 g (47%) of the desired corresponding bromo product.

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

Reference£º
Patent; SOLVAY PHARMACEUTICALS B.V.; US2006/122189; (2006); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem