Day: September 18, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5676-60-8,2-Methylbenzo[d]oxazol-6-amine,as a common compound, the synthetic route is as follows.,5676-60-8

General procedure: In the vessel of a microwave reactor, 12 (400 mg, 1.13 mmol), 2-aminopyridine (318 mg, 3.38 mmol), Pd2(dba)3 (51.6 mg,56.4 lmol), 2-dicyclohexylphosphino-20,40,60-triisopropyl-1,10-biphenyl (26.9 mg, 56.4 lmol), and K2CO3 (312 mg, 2.25 mmol)were suspended in t-BuOH (3 mL). The vessel was then sealed,and the mixture was reacted at 130 C for 1 h under microwaveirradiation. After cooling to room temperature, the mixture wasextracted with CHCl3/MeOH (4:1), and washed with brine. Theorganic layer was separated, dried over MgSO4, and concentratedunder reduced pressure. The residue was purified by NH silicagel column chromatography (CHCl3/MeOH = 100:0 to 90:10) togive the title compound (362 mg, 78%). 1H NMR (400 MHz,DMSO-d6) d: 1.27-1.38 (2H, m), 1.41 (9H, s), 1.95-2.02 (2H, m),2.96-3.10 (2H, m), 3.43-3.53 (1H, m), 3.80-3.88 (2H, m), 6.83-6.87 (1H, m), 7.07 (1H, br), 7.22 (1H, s), 7.62-7.66 (2H, m), 7.80(1H, br), 8.20-8.22 (1H, m), 8.40 (1H, s), 8.70 (1H, d, J = 7.2 Hz),9.47 (1H, s). MS (ESI) m/z: 413 (M+H)+.

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

Reference£º
Article; Nakajima, Yutaka; Aoyama, Naohiro; Takahashi, Fumie; Sasaki, Hiroshi; Hatanaka, Keiko; Moritomo, Ayako; Inami, Masamichi; Ito, Misato; Nakamura, Koji; Nakamori, Fumihiro; Inoue, Takayuki; Shirakami, Shohei; Bioorganic and Medicinal Chemistry; vol. 24; 19; (2016); p. 4711 – 4722;,
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, Step 4 3-Ethoxy-4-(2-oxo-2,3-dihydrobenzooxazol-7-ylamino)cyclobut-3-ene-1,2-dione A mixture of 0.247 g of 7-amino-3H-benzooxazol-2-one (1.6 mmol, 1 eq) and 0.36 ml of 3,4-diethoxycyclobut-3-ene-1,2-dione (2.5 mmol, 1.5 eq) in 9 ml of ethanol was stirred at ambient temperature for 2 days (formation of a precipitate). Ethanol was added in order to promote the fall of the precipitate, which was filtered off, washed with diethyl ether and dried under vacuum at 45 C. 0.35 g of product was obtained in the form of a light khaki solid. Yield=78%.

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; Musicki, Branislav; Aubert, Jerome; Boiteaux, Jean-Guy; Clary, Laurence; Rossio, Patricia; Schuppli-Nollet, Marlene; US2014/309208; (2014); 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, 128156-54-7 Methyl benzo[d]oxazole-4-carboxylate 14616761, abenzoxazole compound, is more and more widely used in various fields.

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

177492-52-3, Benzo[d]oxazol-6-amine is a benzoxazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixture of the appropriate amine (1M-3M, 2 mmol) and the appropriate aldehyde (2.2 mmol) in ethanol (10 mL) was stirred at room temperature for 8 h., 177492-52-3

177492-52-3 Benzo[d]oxazol-6-amine 584120, abenzoxazole compound, is more and more widely used in various fields.

Reference£º
Article; Zhang, Da-Jun; Sun, Wen-Fang; Zhong, Zhao-Jin; Gao, Rong-Mei; Yi, Hong; Li, Yu-Huan; Peng, Zong-Gen; Li, Zhuo-Rong; Molecules; vol. 19; 1; (2014); p. 925 – 939;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

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

General procedure: To a solution of 4-chloro-6-methylpyrimidin-2-amine (1)(1 mmol) in dry ethanol (4 ml), benzoxazol-2-amine (2a)/benzothiazol-2-amine (2b)/1H-benzimidazol-2-amine (2c)(1.1 mmol) and a catalytic amount of methanesulfonic acid(0.2 ml) were added and refluxed for 5?7 h. After completionof the reaction the contents were cooled and dilutedwith water (15 ml). The separated solid was filtered, washedwith water, dried and recrystallized from 2-propanol. N4-(1,3-Benzoxazol-2-yl)-6-methyl-2,4-pyrimidinediamine(4a)Red solid; yield 74percent; m.p. 138?140 ¡ãC; IR (KBr) vmax 3478(NH2), 3381, 3320 (NH), 1578 (C=N) cm?1; 1H NMR(DMSO?d6, 400 MHz): delta = 2.47 (s, 3H, CH3), 7.01 (s, 1H,C5?H), 7.12 (s, 2H, NH2), 7.33?7.49 (m, 4H, Ar?H), 8.27(bs, 1H, NH); 13C NMR (DMSO?d6, 100 MHz): delta = 24.9(CH3), 96.1 (C?5), 160.4 (C?2?), 164.4 (C?2), 167.5 (C?6),171.9 (C?4), 112.3, 121.6, 125.9, 126.7, 143.4, 152.5(aromatic carbons); MS (m/z): 241.25 [M+]. Anal. Calcd.for C12H11N5O: C, 59.74; H, 4.60; N, 29.03. Found: C,59.86; H, 4.62; N; 29.24.

The synthetic route of 4570-41-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Seenaiah, Dandu; Rekha, Tamatam; Padmaja, Adivireddy; Padmavathi, Venkatapuram; Medicinal Chemistry Research; vol. 26; 2; (2017); p. 431 – 441;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.64037-15-6,5-Methyl-2-aminobenzoxazol,as a common compound, the synthetic route is as follows.,64037-15-6

To a 50 ml three-necked flask was added 5-methylbenzoxazol-2-amine, 10 ml of tetrahydrofuran, 5 ml of triethylamine. The acid chloride was then dissolved in 10 ml of dry tetrahydrofuran, Below 5 deg C under the conditions of slow drop, The reaction was stirred at room temperature for 4 h. 40 ml of saturated aqueous sodium chloride solution was added,The aqueous phase was extracted three times with 25 ml of dichloromethane, Combine the organic phase. Column separation, Dichloromethane: methanol 60: 1 to give 1.39 g of a white solid, M.p. 174 to 176 C, yield: 70.6%.

The synthetic route of 64037-15-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences; Si, Shuyi; Gao, Nana; Jiang, Wei; Jiang, Jiandong; Li, Yan; Li, Dongsheng; Li, Yongzhen; Zhang, Jing; Zhu, Ningyu; Wang, Zhimin; (20 pag.)CN103772376; (2017); B;,
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,4570-41-6

General procedure: To a solution of carboxylic acid 3 in 3 mL dimethylformamide,were added trimethylamine (3 equiv), EDCI (1.2 equiv) and HOBt( 1.2 equiv) under ice-bath. After stirring at room temperature for30 min, amines (1 equiv) were added and the resulting mixture stirred for 24 h at room temperature. Reaction was detected byTLC (EtOAc/Hex 2:1). After completion of reaction, the mixture was diluted with water and extracted with ethyl acetate. The combined organic layers were washed by brine, dried over MgSO4 and concentrated. The crude product was further purified by silica gel chromatography eluted with EtOAc/Hex 2:1 to afford pure desired compound. 4.1.3.8 N-(Benzoxazol-2-yl)-5-(4-(4-chlorophenyl)piperazin-1-yl)pentanamide (4h¡¤HCl) The compound 4h was prepared from 3c and 2-aminobenzoxazole as a colorless solid (yield: 24.7percent). The free base was further converted into 4h¡¤HCl as a white solid. Mp: 78-79 ¡ãC. 1H NMR (300 MHz, DMSO-d6) delta 11.19 (s, 1H), 9.80 (s, 2H), 7.59 (d, J = 7.7 Hz, 1H), 7.40 (dd, J = 7.7, 1.2 Hz, 1H), 7.36-7.19 (m, 4H), 7.01 (d, J = 9.0 Hz, 2H), 3.78 (d, J = 12.1 Hz, 2H), 3.50 (d, J = 10.9 Hz, 2H), 3.14 (m, 6H), 2.37 (t, J = 7.3 Hz, 2H), 1.75 (m, 2H), 1.63-1.47 (m, 2H).

The synthetic route of 4570-41-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Cao, Yongkai; Paudel, Suresh; Zhang, Xiaowei; Kim, Kyeong-Man; Cheon, Seung Hoon; Bioorganic and Medicinal Chemistry; vol. 23; 17; (2015); p. 5264 – 5272;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

64037-15-6,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.64037-15-6,5-Methyl-2-aminobenzoxazol,as a common compound, the synthetic route is as follows.

A solution of succinic anhydride (141.1 g, 1.41 mol) and 70 g (about 0.47 mol) of compound of step 1a (70 g, 0.47 mol) in 2500 ml of anhydrous toluene was refluxed for overnight. After that, HATU (100 g, 0.26 mol) and 4-methylmorpholine (41.36 ml, 0.376 mol) were added and the resulting mixture was refluxed for 2-3 hours. TLC showed that the major spot was product (Rf=0.35, acetone_hexane=1:2). After reaction was completed, the solvent was evaporated and the residue was dissolved in about 2000 ml of CH2Cl2. The solution was washed with aqueous NaHCO3. After pH was adjusted to 7-8 and washed with brine, organic phase was separated and dried over MgSO4. Filtration and removal of solvent gave the title compound (98 g) as fine white needle crystalline

64037-15-6 5-Methyl-2-aminobenzoxazol 46388, abenzoxazole compound, is more and more widely used in various fields.

Reference£º
Patent; Wang, Guoqiang; Phan, Ly Tam; Or, Yat Sun; Qiu, Yao-ling; Niu, Deqiang; Peng, Yulin; Busuyek, Marina; Wang, Yanchun; Nakajima, Suanne; US2006/252712; (2006); A1;,
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 33 N-Benzooxazol-2-yl-3-cyclopentyl-2-(4-methanesulfonyl-3-nitro-phenyl)-propionamide A solution of 3-cyclopentyl-2-(4-methanesulfonyl-3-nitrophenyl)-propionic acid (prepared as in Example 32, 50 mg, 0.15 mmol), triethylamine (0.060 mL, 0.44 mmol), benzotriazol-1-yloxy-tris(dimethylamino)phosphonium hexafluorophosphate (98 mg, 0.22 mmol), and 2-aminobenzoxazole (30 mg, 0.22 mmol) in N,N-dimethylformamide (3 mL) was stirred at 25¡ã C. for 3 h. The reaction mixture was then diluted with water (25 mL), a 1N aqueous hydrochloric acid solution (5 mL), and ethyl acetate (25 mL). The layers were separated. The resulting organic layer was washed with a saturated aqueous sodium chloride solution (1*25 mL), dried over magnesium sulfate, filtered, and concentrated in vacuo. Flash chromatography (Merck Silica gel 60, 230-400 mesh, 2/1 hexanes/ethyl acetate) afforded N-benzooxazol-2-yl-3-cyclopentyl-2-(4-methanesulfonyl-3-nitro-phenyl)-propionamide (13 mg, 19.5percent) as a yellow solid: mp 106-110¡ã C.; EI-HRMS m/e calcd for C22H23N3O6S (M+) 457.1308, found 457.1323.

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; Corbett, Wendy Lea; Grimsby, Joseph Samuel; Haynes, Nancy-Ellen; Kester, Robert Francis; Mahaney, Paige Erin; Sarabu, Ramakanth; US2002/103199; (2002); 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 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