Tag: 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

2-Bromopyridine (1 ) (1 .0g, 6.3mmol), benzo[d]oxazol-2-amine (2) (0.871 g, 6.4mmol), Xantphos (0.37g, 0.63mmol), and Cs2C03 (3.09g, 9.4mmol) were combined in dry 1 ,4-dioxane (15mL). The reaction mixture was degassed with N2(g) and placed under vacuum for 10min. Pd2(dba)3 (0.289g, 0.31 mmol) was then added and the resulting reaction mixture was heated at 90¡ãC for 30h. It was then poured onto demineralized water (200ml_), and extracted with EtOAc (3 x 100ml_). The organic phases were combined, dried over Na2S04, filtered and subsequently concentrated in vacuo. The resulting residue was purified by flash chromatography with EtOAc/Hexane (1 : 1 ) to provide N-(pyridin-2- yl)benzo[d]oxazol-2-amine (3) as a yellow solid (0.8g, 60percent). LCMS (ES): Found 212.1 [M+H]+

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

Reference£º
Patent; KARUS THERAPEUTICS LTD; SHUTTLEWORTH, Stephen Joseph; WHALE, Andrew David; (145 pag.)WO2017/29514; (2017); 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

General procedure for the preparation of intermediates of the General Formula (9)Intermediate (9) A mixture of benzaldehyde derivative (1.0 equiv.) and 2-aminobenzoxazole or 2- aminobenzothiazole (1.0 equiv.) in ^-xylene was stirred at reflux temperature for 18 h. The mixture containing the imino derivative was cooled to room temperature and sodium cyanoborohydride (1.2 equiv.) was added over 5 min. The reaction mixture was then further stirred at room temperature for 48 h. The mixture was diluted with ethyl acetate and washed twice with water. The organic layer was dried and evaporated to give a viscous residue, which was purified by silica gel column chromatography to yield the compound of general formula (9) as off-white to yellow solid.

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

Reference£º
Patent; GLENMARK PHARMACEUTICAL S.A.; IRLAPATI, Nagoswara, Rao; THOMAS, Abraham; KURHE, Deepak, Kantilal; SHELKE, Sandeep, Yadunath; KHAIRATKAR, JOSHI, Neelima; VISWANADHA, Srikant; MUKHOPADHYAY, Indranil; WO2010/10435; (2010); A2;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

Benzo[d]oxazol-2-amine, cas is 4570-41-6, it is a common heterocyclic compound, the benzoxazole compound, its synthesis route is as follows.,4570-41-6

2-Bromo-5-fluoropyridine (1) (lOg, 5.7lmmol), benzo[d]oxazol-2-amine (2) (766mg, 5.7lmmol), Xantphos (0.33g, 0.S7mmol), and Cs2003 (2.79g, 8.S6mmol) were combined in dry 1,4-dioxane (l5mL). The reaction mixture was degassed with N2(g) and placed under vacuum for 10mm. Pd2(dba)3 (0.261g, 0.28mmol) was then addedand the resulting reaction mixture was heated at 9000 for 30h. It was then poured onto demineralized water (200mL), and extracted with EtOAc (3 x lOOmL). The organic phases were combined, dried over Na2SO4, filtered and subsequently concentrated in vacuo. The resulting residue was purified by flash chromatography with EtOAc/Hexane (1:1) to provide N-(5-fluoropyridin-2-yl)benzo[d]oxazol-2-amine(3) as a yellow solid (0.6g, 46percent).LCMS (ES): Found 230.1 [M+H].

With the rapid development of chemical substances, we look forward to future research findings about 4570-41-6

Reference£º
Patent; KARUS THERAPEUTICS LTD; SHUTTLEWORTH, Stephen Joseph; TOMASSI, Cyrille Davy; CECIL, Alexander Richard Liam; MACCORMICK, Somhairle; NODES, William John; SILVA, Franck Alexandre; WO2014/181137; (2014); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

4570-41-6,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4570-41-6,Benzo[d]oxazol-2-amine,as a common compound, the synthetic route is as follows.

General procedure: A mixture of 6a/6b/6c/7a/7b/7c (1 mmol),benzoxazol-2-amine (2a)/benzothiazol-2-amine (2b)/1Hbenzimidazol-2-amine (2c)/(benzoxazol-2-yl)methanamine(3a)/(benzothiazol-2-yl) methanamine (3b)/(1H-benzimidazol-2-yl)methanamine (3c) (1.1 mmol), dry ethanol (4 ml)and a catalytic amount of methanesulfonic acid (0.2 ml) wasrefluxed for 6?7 h. The contents of the flask were cooledand diluted with water (15 ml). The separated solid wasfiltered, washed with water, dried and recrystallized from 2-propanol. N-(1,3-Benzoxazol-2-yl)-N?-[4-(1,3-benzoxazol-2-ylamino)-6-methyl-2-pyrimidinyl]sulfamide (9a)Red solid; yield (method A 65percent and method B 84percent); m.p.175?177 ¡ãC; IR (KBr) vmax 3367 (NH), 1583 (C=N), 1333(SO2), 1163 cm?1; 1H NMR (DMSO?d6, 400 MHz): delta =2.67 (s, 3H, CH3), 7.38 (s, 1H, C5?H), 7.47?7.69 (m, 8H,Ar?H), 8.45 (bs, 1H, NH?C2?), 8.63 (bs, 1H, NH?C2?), 8.70(bs, 1H, C2?NH); 13C NMR (DMSO?d6, 100MHz): delta =27.1 (CH3), 97.6 (C?5), 154.6 (C?2?), 161.3 (C?2?), 168.4(C?6), 171.3 (C?2), 172.3 (C?4), 113.3, 113.7, 122.6,122.9, 126.5, 126.8, 127.4, 127.9, 143.9, 144.4, 153.3, 153.8 (aromatic carbons); MS (m/z): 437.45 [M+]. Anal.Calcd. for C19H15N7O4S: C, 52.17; H, 3.46; N, 22.41.Found: C, 52.29; H, 3.50; N, 22.58.

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

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

Benzo[d]oxazol-2-amine, cas is 4570-41-6, it is a common heterocyclic compound, the benzoxazole compound, its synthesis route is as follows.,4570-41-6

Step 1:To a solution of 4-fluorophenylacetic acid (1.0 g, 6.5 mmol) and 2-amino-benzoxazole (850 mg, 6.5 mmol) in CH2Cl2 (50 mL) was added DMAP (237 mg, 1.9 mmol) and EDC.HCl (1.5 g, 7.8 mmol).The reaction mixture was stirred at room temperature over night.The reaction mixture was concentrated in vacuo.Purification by chromatography (silica, 30percent ethyl acetate/CH2Cl2) afforded N-benzooxazol-2-yl-2-(4-fluorophenyl)acetamide (1.44 g, 82percent): 1H NMR (300 MHz, DMSO-d6) delta ppm 3.85 (s, 2H) 7.11-7.21 (m, 2H) 7.23-7.44 (m, 4H) 7.52-7.69 (m, 2H).

With the rapid development of chemical substances, we look forward to future research findings about 4570-41-6

Reference£º
Patent; Brotherton-Pleiss, Christine E.; Walker, Keith A. M.; US2012/149718; (2012); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

Benzo[d]oxazol-2-amine, cas is 4570-41-6, it is a common heterocyclic compound, the benzoxazole compound, its synthesis route is as follows.,4570-41-6

Example 66: 4-r3-(4-Chloro-phenoxy)-benzyl1-piperazine-1 -carboxylic acid benzooxazol-2-ylamide.; To a solution of benzooxazole-2-ylamine (35.8 mg, 0.267 mmol) in CH2CI2 (6.0 ml_) was added N,N’-disuccinimidyl carbonate (68.4 mg, 0.267 mmol). The reaction mixture was stirred at rt for 6 h, then treated with 1-[3-(4-chloro-phenoxy)- benzyl]-piperazine hydrochloride (100 mg, 0.267 mmol) and diisopropylethylamine (92 mul_, 0.536 mmol) and stirred for an additional 16 h at rt. The reaction mixture was diluted with EtOAc (100 ml_) and extracted with H2O (100 ml_) then saturated aqueous NaCI (50 ml_). The organic layer was dried (MgSO4), and concentrated. The crude residue was purified (FCC, 2 N NH3 in MeOH/DCM) to give 4-[3-(4-chloro- phenoxy)-benzyl]-piperazine-1 -carboxylic acid benzooxazol-2-ylamide (78.0 mg, 63percent). MS (ESI+): calcd for C25H23CIN4O3 m/z 462.15, found 463.5 (M+H)+. 1H NMR (d6-DMSO): 12.13 (br s, 1 H), 7.46-7.39 (m, 3H), 7.36 (t, J = 7.9, 1 H), 7.30 (br s, 1 H), 7.22 (t, J = 7.6, 1 H), 7.18-7.11 (m, 2H), 7.04 (d, J = 9.0, 2H), 7.00 (br s, 1 H), 6.94- 6.91 (m, 1 H), 3.73-3.54 (br m, 4H), 3.50 (s, 2H), 2.40-2.31 (m, 4H).

With the rapid development of chemical substances, we look forward to future research findings about 4570-41-6

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;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

Benzo[d]oxazol-2-amine, cas is 4570-41-6, it is a common heterocyclic compound, the benzoxazole compound, its synthesis route is as follows.,4570-41-6

2-Bromo-5-fluoropyridine (1 ) (1 .0g, 5.71 mmol), benzo[d]oxazol-2-amine (2) (766mg, 5.71 mmol), Xantphos (0.33g, 0.57mmol), and Cs2C03 (2.79g, 8.56mmol) were combined in dry 1 ,4-dioxane (15mL). The reaction mixture was degassed with N2(g) and placed under vacuum for 10min. Pd2(dba)3 (0.261 g, 0.28mmol) was then added and the resulting reaction mixture was heated at 90¡ãC for 30h. It was then poured onto demineralized water (200ml_), and extracted with EtOAc (3 x 100ml_). The organic phases were combined, dried over Na2S04, filtered and subsequently concentrated in vacuo. The resulting residue was purified by flash chromatography with EtOAc/Hexane (1 : 1 ) to provide N-(5-fluoropyridin-2-yl)benzo[d]oxazol-2-amine (3) as a yellow solid (0.6g, 46percent). LCMS (ES): Found 230.1 [M+H]+

With the rapid development of chemical substances, we look forward to future research findings about 4570-41-6

Reference£º
Patent; KARUS THERAPEUTICS LTD; SHUTTLEWORTH, Stephen Joseph; WHALE, Andrew David; (145 pag.)WO2017/29514; (2017); 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

Step 1:To a solution of 4-methylsulfonylphenylacetic acid (214 mg, 1 mmol) and 2-amino-benzoxazole (147 mg, 1.1 mmol) in CH2Cl2 (10 mL) was added DMAP (37 mg, 0.3 mmol) and EDC.HCl (230 mg, 1.2 mmol).The reaction mixture was stirred at room temperature for 6 h.The reaction mixture was concentrated in vacuo.Purification by chromatography (silica, 10-75percent ethyl acetate/hexanes gradient) afforded N-benzooxazol-2-yl-2-(4-methanesulfonyl-phenyl)acetamide (175 mg, 53percent): LC/MS-ESI observed [M+H]+ 331.

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

Reference£º
Patent; Brotherton-Pleiss, Christine E.; Walker, Keith A. M.; US2012/149718; (2012); 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.4570-41-6,Benzo[d]oxazol-2-amine,as a common compound, the synthetic route is as follows.

General procedure: Oxazolone (2; 0.251 mmol, 1 eq) and amine nucleophile(0.326 mmol, 1.3 eq) was dissolved in toluene (1 mL) to aconcentration of 0.251 M. The reaction mixture was stirredat 70 C for 3 h, and concentrated in vacuo. The residuewas purified by flash column chromatography on silica gelusing n-heptane/EtOAc as the eluents to afford compound.

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

Reference£º
Article; Jo, Minmi; Won, Sun-Woo; Lee, Dong Guk; Yun, Jungeon; Kim, Sunhong; Kwak, Young-Shin; Archives of Pharmacal Research; vol. 41; 5; (2018); p. 481 – 489;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4570-41-6,Benzo[d]oxazol-2-amine,as a common compound, the synthetic route is as follows.

(Step 1) Synthesis of (R)-tert-butyl 3-(4-amino-3-((benzo[d]oxazol-2-yl)carbamoyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate (0190) 300 mg of (R)-tert-butyl 3-(4-amino-3-iodo-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate obtained in Reference Example 1 was dissolved in 3 mL of NMP. 118 mg of benzo[d]oxazol-2-amine, 20 mg of xantphos, and 0.15 mL of N-methylmorpholine were added thereto, and a degassing operation was carried out. Thereafter, 7.6 mg of palladium acetate was added thereto, and under a carbon monoxide atmosphere, the mixture was heated to 110¡ã C. and stirred for 2 hours. After the mixture was cooled, 4.5 mL of methanol and 0.45 mL of a 5 N aqueous solution of sodium hydroxide were added thereto, and the mixture was stirred for 30 minutes at room temperature. Thereafter, the pH was adjusted to 5.3 with 2 N HCl, and a solid thus obtained was collected by filtration. The crude product was purified by a silica gel column (chloroform-methanol), and thus 257 mg of the title compound was obtained as a white solid.

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

Reference£º
Patent; TAIHO PHARMACEUTICAL CO., LTD.; OSHIUMI, Hiromi; (27 pag.)US2017/44166; (2017); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem