Day: September 23, 2020

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.

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].

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; 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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.19932-85-5,6-Bromobenzo[d]oxazol-2(3H)-one,as a common compound, the synthetic route is as follows.

19932-85-5, To a solution of XXXV-2b (500 mg, 2.97 mmol) in dry DCM (20 mL) was added TEA (360 mg, 3.56 mmol) and Trt-Cl (992 mg, 3.56 mmol). The mixture was stuffed overnight at rt, then poured into water, extracted with DCM (50 mLx3). The combined organic layer was washed with brine, dried over anhydrous Na2SO4, and concentrated in vacuo. The residue was purified by column chromatography on silica gel (PE/EA=10/1) to afford XXXV-3b (1.2 g, 89% yield).

As the paragraph descriping shows that 19932-85-5 is playing an increasingly important role.

Reference£º
Patent; INTERMUNE, INC.; RAMPHAL, Johnnie, Y.; BUCKMAN, Brad, Owen; EMAYAN, Kumaraswamy; NICHOLAS, John, Beamond; SEIWERT, Scott, D.; WO2015/153683; (2015); 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.1086378-35-9,Methyl benzo[d]oxazole-7-carboxylate,as a common compound, the synthetic route is as follows.

Methyl benzo[d]oxazole-7-carboxylate (1.57 g, 8.86 mmol) was dissolved in dry THF (50 mL) and there was added a 1.0M solution of LiAlH4 in THF (5mL, 5 mmol). The reaction was stirred at room temperature for 30 minutes at which point TLC indicated full conversion. The reaction was quenched by addition of water (50 mL) and there was added saturated aqueous Rochelle salt (50 mL) and Et2O (50 mL). The reaction was stirred vigorously for 15 minutes and then transferred to a separatory funnel. The organic layer was isolate and the aqueous layer was extracted with Et2O (2 ¡Á 100 mL). The combined organic layers were washed with saturated aqueous Rochelle salt (50 mL) and water (50 mL), dried (MgSO4), filtered and evaporated under reduced pressure. The crude compound was purified by flash chromatography (petroleum ether/EtOAc 3:1) to give the title compound (0.823 g, 62%) as a colorless oil. 1H NMR (300 MHz, CDCl3) delta 8.07 (s, 1H), 7.69 (dd, J = 7.7, 1.3 Hz, 1H), 7.40 (dd, J = 7.7, 1.3 Hz, 1H), 7.33 (t, J = 7.7 Hz), 5.00 (s, 2H), 2.51 (br s, 1H). 13C NMR (75 MHz, CDCl3) delta 153.4, 145.4, 140.0, 124.8, 124.7, 124.4, 119.9, 60.3, 1086378-35-9

The synthetic route of 1086378-35-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Hansen, Martin; Jacobsen, Stine Engesgaard; Plunkett, Shane; Liebscher, Gudrun Eckhard; McCorvy, John D.; Braeuner-Osborne, Hans; Kristensen, Jesper Langgaard; Bioorganic and Medicinal Chemistry; vol. 23; 14; (2015); p. 3933 – 3937;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.19932-85-5,6-Bromobenzo[d]oxazol-2(3H)-one,as a common compound, the synthetic route is as follows.

Intermediate 13: 2-oxo-2,3-dihydrobenzo[d]oxazole-6-carbonitrile To a solution of 6-bromo benzoxazolinone (2 g, 9.4 mmol) in DMF (20 mL) was added CuCN (16.79 g, 188 mmol), and the reaction was stirred at 175 C. for 6 h. The reaction progress was monitored by TLC (100% EtOAc). The reaction was diluted with EtOAc (10 mL) and filtered through Celite brand filter agent. The organic layer was concentrated and purified by column chromatography (silica gel, 0-50% EtOAc in hexanes) to give the title compound. MS (ESI pos. ion) m/z: 158.9 (MH-)., 19932-85-5

19932-85-5 6-Bromobenzo[d]oxazol-2(3H)-one 29859, abenzoxazole compound, is more and more widely used in various fields.

Reference£º
Patent; AMGEN INC.; BISWAS, Kaustav; CHEN, Jian J.; GORE, Vijay Keshav; HARRIED, Scott; HORNE, Daniel B.; KALLER, Matthew R.; MA, Vu Van; SHAM, Kelvin; ZHONG, Wenge; US2014/45855; (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.5676-60-8,2-Methylbenzo[d]oxazol-6-amine,as a common compound, the synthetic route is as follows.

5676-60-8, General procedure: To a solution of compound 3 (3.37 mmol) in DMF (10 mL), charged respective compound V (a-p) (4.04 mmol) and heated to 80 C. After3 h, TLC analysis showed complete conversion of starting materials. The reaction mixture was cooled to room temperature, charged water (30 mL) and extracted with EtOAc (2 ¡Á 20 mL). The combined organic layer was washed with water (20 mL) followed by brine and concentrated under reduced pressure to obtain gummy liquid. This crude material was triturated with MTBE to afford desired product as solid and which used as such in next step without any further purification.

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

Reference£º
Article; Balraju, Vadla; Jogula, Sridhar; Krishna, Vagolu Siva; Meda, Nikhila; Sriram, Dharmarajan; Bioorganic Chemistry; vol. 100; (2020);,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.54903-16-1,2-Oxo-2,3-dihydrobenzo[d]oxazole-6-carboxylic acid,as a common compound, the synthetic route is as follows.

54903-16-1, To a stirred solution of 2-oxo-2,3-dihydrobenzo[d]oxazole-6-carboxylic acid (0.2 g, 0.66 mmol) in DMF (1.5 mL) was added EDCI.HCl (0.191 g, 1.00 mmol), HOBt (0.091 g, 0.66 mmol) and diispropylethylamine (0.34 mL, 2.00 mmol). The solution was stirred for 10 min at 0oC. After that, tert-butyl ((2S)-1-(4-(1-aminoethyl)piperidin-1-yl)- 1-oxopropan-2-yl)carbamate (0.142 g, 0.80 mmol) was added and the reaction stirred at rt for 12 h. The progress of the reaction was monitored by TLC. After complete consumption of starting material, the reaction was quenched with water and extracted with ethyl acetate. The organic layer was separated, washed with brine, dried over anhydrous Na2SO4and concentrated under reduced pressure to obtain a crude residue which was purified by column chromatography to afford tert-butyl ((2S)-1-oxo-1-(4-(1- (2-oxo-2,3-dihydrobenzo[d]oxazole-6-carboxamido)ethyl)piperidin-1-yl)propan-2- yl)carbamate (0.104 g, 33%)

54903-16-1 2-Oxo-2,3-dihydrobenzo[d]oxazole-6-carboxylic acid 391472, abenzoxazole compound, is more and more widely used in various fields.

Reference£º
Patent; Epizyme, Inc.; Poley, Megan Allen Clunan; Kunz, Kevin Wayne; Mills, James Edward John; Mitchell, Lona Helen; munckhof, Michael John; Harvey, Darren Martin; (303 pag.)KR2017/45749; (2017); A;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

13451-78-0, 5-Fluorobenzo[d]oxazole-2-thiol is a benzoxazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 2 The 2-mercapto-5-fluorobenzoxazole (2.0 g, 11.8 mmol) is slurried into POCl3 (9.7 mL, 104 mmol). The slurry is treated with PCl5 (3.0 g, 14.2 mmol) and 5.0 mL of anhydrous CH2 Cl2. The mixture is stirred at room temperature for 5.5 hours. After this time excess POCl3 is removed under reduced pressure. The residue is treated with saturated aqueous NaHCO3 and the mixture is poured into a separatory funnel. The mixture is extracted with EtOAc and the combined extracts are washed with brine and dried over anhydrous Na2 SO4. Filtration and concentration gives 1.76 g of 2-chloro-5-fluorobenzoxazole as a waxy solid. The crude chloride is used in the piperazine displacement reaction., 13451-78-0

The synthetic route of 13451-78-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Pharmacia & Upjohn Company; US5736545; (1998); 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.73101-74-3,2-(Bromomethyl)benzo[d]oxazole,as a common compound, the synthetic route is as follows.,73101-74-3

General procedure: Pyridine derivative (0.2 mmol) was dissolved in dichloromethane(2 mL) and benzyl bromide derivative (1.2e2.0 equiv) wasthen added and the solutionwas heated to 50 C for 12 h in a sealedtube. After cooling at room temperature and concentration underreduced pressure, the resulting solid was triturated in diethyl ether,filtered and rinsed with diethyl ether to afford the compounds13e21, 33 and 41.

The synthetic route of 73101-74-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Azzouz, Rabah; Peauger, Ludovic; Gembus, Vincent; ?in?a?, Mihaela-Liliana; Papamicael, Cyril; Levacher, Vincent; Sopkova-de Oliveira Santos, Jana; European Journal of Medicinal Chemistry; vol. 145; (2018); p. 165 – 190;,
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

To a suspension of benzo[d]oxazol-2-amine (5.Og, 37.3mmol) in DMF (5OmL) was added 20.0 M NaOH (1.86mL, 37.3mmol) at 0 00. The reaction mixture was stirred for 10 mm and CS2 (6.32mL, 93.2mmol) was added dropwise at 0 00 and the reaction mixture was further stirred for 10 mm at 0 00 An additional portion of 20.0 M NaOH (1.86mL, 37.3mmol) was added at 0 00 and reaction mixture was again stirred for 10 mm at 0 00 Finally, CH3I (5.84mL, 93.2mmol) was added dropwise at 0 00. The reaction mixture was stirred at rt for 30 mm. The TLC showed reaction to be complete. The mixture was poured into ice-water (lOOmL) and the precipitated solid was filtered , washed with water(5OmL) followed by hexane (3OmL) and dried under reduced pressure to obtain dimethyl benzo[d]oxazol-2- ylcarbonimidodithioate as an off white solid . Yield: 6.92g (78percent). MS (ESl+) for CHNOS m/z 239.03 [M+H] 1H NMR (400 MHz, DMSO-d6): 7.64 (bs, 2H), 7.32 (bs, 2H), 2.67 (bs, 6H).

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; DISCUVA LTD.; MEO, Dr Paul; KHAN, Dr. Nawaz; (284 pag.)WO2018/37223; (2018); 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.5676-60-8,2-Methylbenzo[d]oxazol-6-amine,as a common compound, the synthetic route is as follows.,5676-60-8

To a solution of 3-chloro-2-methylbenzenesulphonyl chloride (163 mg, 0.723 MMOL) in dichloromethane (3 mL) was added pyridine (140 pL, 1.72 MMOL) and the mixture was stirred under N2 for 5 min, after which time 6-amino-2-methylbenzoxazole (102 mg, 0.688 MMOL) was added. The resulting mixture was stirred for 1 h at room temperature, then saturated NAHC03 solution was added (8 mL) and the mixture was extracted into ethyl acetate (15 mL). The organic phase was washed with brine, dried (Na2SO4), filtered and evaporated to give a residue that was purified using flash chromatography to afford a white solid (151 mg, 65%), single spot at Rf 0.50 (60: 40 hexane: ethyl acetate). mp 127.1-127. 5C, HPLC purity 97% (tR 2.05 min in 10% WATER-ACETONITRILE). 1H NMR (CDCl3) : O 7.85 (1H, dd, J=8.1, 1.1 Hz), 7.53 (1H, dd, J=8.1, 1.3 Hz), 7.45 (1H, d, J=8. 4 Hz), 7.27 (1H, d, J=2.2 Hz), 7.17 (1H, t, J=7.9 Hz), 6.93 (1H, s, N-H), 6.86 (1H, dd, J=8.4, 2.2 Hz), 2.71 (3H, s), 2.58 (3H, s). LCMS: 335.14 (M-). FAB-MS (MH+, C15H13CIN203S) : calcd 337.0413, found 337.0406.

As the paragraph descriping shows that 5676-60-8 is playing an increasingly important role.

Reference£º
Patent; STERIX LIMITED; WO2004/37251; (2004); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem