Month: September 2020

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.

A solution of methyl benzo[d]oxazole-7-carboxylate (0.5 g, 2.82 mmol), 1-iodo-4-nitrobenzene (0.88 g, 3.53 mmol), lithium tert-butoxide (0.45 g, 5.64 mmol), tetrakis(triphenyl phosphine)palladium(0) (0.16 g, 0.141 mmol) in dioxane under a nitrogen atmosphere was stirred at room temperature for 45 minutes. The resulting thick suspension was diluted with EtOAc, washed with water, organics washed with brine, dried over Na2SO4, decanted and solvent removed under vacuum. The crude was purified by column chromatography on silica gel using 20:1 to 5:1 Hexane:EtOAc as eluent to give methyl 2-(4-nitrophenyl)benzo[d]oxazole-7-carboxylate (0.4 g, 48%). UPLC-MS (Acidic Method, 2 min): rt 1.11 min, m/z 299.0 [M+H]+, 1086378-35-9

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

Reference£º
Patent; JAGUAHR THERAPEUTICS PTE LTD; METE, Antonio; HITCHIN, James, R.; GRAHAM, Mark; (46 pag.)WO2020/43880; (2020); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

22876-19-3, 5-Chlorobenzo[d]oxazole-2(3H)-thione is a benzoxazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Oxalyl chloride (1.20 g, 9.4 mmol) was added dropwise to a stirred suspension of 2- mercapto-5-chlorobenzoxazol (1.28 g, 6.9 mmol) in CH2C12(37 mL) at The solution of 2,5-Dichlorobenzoxazol was added to a solution of (7-Methyl-l ,4- diazepan-l-yl)(5-methyl-2-(2H-l ,2,3-triazol-2-yl)phenyl)methanone (1.88 g, 6.3 mmol) and NEt3(3.18 g, 6.3 mmol) in DMF (24 mL) at room temperature. The reaction mixture was then stirred at 70 C for 19 hours and at 90 C for 20 hours. The reaction mixture was then cooled to room temperature and quenched with a saturated solution of NaHC03(50 mL). The organic phase was separated and washed with H20 (50 mL) followed by brine (50 mL). The organic phase was dried over MgS04, filtered and concentrated to give crude Suvorexant (3.58 g)., 22876-19-3

22876-19-3 5-Chlorobenzo[d]oxazole-2(3H)-thione 708870, abenzoxazole compound, is more and more widely used in various.

Reference£º
Patent; SANDOZ AG; BARTH, Roland; KAUFMANN, Marius; (97 pag.)WO2016/20404; (2016); 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

6-Bromobenzo[d]oxazol-2(3H)-one, cas is 19932-85-5, it is a common heterocyclic compound, the benzoxazole compound, its synthesis route is as follows.,19932-85-5

A mixture of 6-bromo-1 ,3-benzoxazol-2(3H)-one (2 g ; 9.34 mmol) and copper (I ) cyan ide (1 .42 g; 1 5.86 mmol) in 6 m l D M F is heated at 1 50C u nder nitrogen atmosphere for 22 hr. After cooling to room temperature, a solution of 1 .55 g (31 .6 mmol) of sodium cyanide in 32 ml water is added followed by 1 hr stirring. The system is extracted thoroughly with ethyl acetate, washed with brine, dried and concentrated in vacuo to provide 1 .5 g (93 % yield) of the title compound enough pure as to prosecute the syntesis.

With the rapid development of chemical substances, we look forward to future research findings about 19932-85-5

Reference£º
Patent; ALMIRALL, S.A.; AIGUADE BOSCH, Jose; GUAL ROIG, Silvia; PRAT QUINONES, Maria; PUIG DURAN, Carlos; WO2013/68552; (2013); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

Methyl 2-mercaptobenzo[d]oxazole-6-carboxylate, cas is 72752-81-9, it is a common heterocyclic compound, the benzoxazole compound, its synthesis route is as follows.,72752-81-9

Methyl 2-chloro-l,3-benzoxazole-6-carboxylate (Intermediate B) To Compound4 (2 g, 9.5 mmol), SOCl2 (9.8 ml, 134 mmol) and DMF (0.8 niL, 10 mmol) was added at room temperature. The reaction mixture heated to reflux for 15 min. The solvent was removed under reduced pressure. The crude oil was azeotroped with xylene twice. The residue was dissolved in a minimum amount of DCM / MeOH, and then loaded onto a silica gel column, eluting with EtOAc/isohexane to give intermediate B as a white solid. H NMR (500MHz, CDC13, ppm): 4.0 (s, 3H)5 7.8 (d, IH), 8.1 (d, IH), 8.3 (s, IH). LC-MS, M+l – 212.1

With the rapid development of chemical substances, we look forward to future research findings about 72752-81-9

Reference£º
Patent; MERCK SHARP & DOHME CORP.; HE, Jiafang; BAWIEC, John; LIU, Weiguo; LIANG, Gui-Bai; YANG, Lihu; WO2010/56717; (2010); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

5-Fluoro-2-methylbenzo[d]oxazole, cas is 701-16-6, it is a common heterocyclic compound, the benzoxazole compound, its synthesis route is as follows.,701-16-6

General procedure: The SBOs were prepared by the base-catalysed condensation of the appropriate 5-halogeno-2-methylbenzoxazole with the requisite aromatic aldehyde under phase transfer conditions. In a typical experiment, equimolar quantities (5 mmol) of the starting materials were dissolved in dichloromethane (20-50 ml) in the presence of benzyltriethylammonium chloride (3 mmol) and stirred magnetically under a nitrogen atmosphere as an aqueous solution of sodium hydroxide (50%, w/v, 5 ml) was added dropwise over a period of 10 min. After being stirred for 2-36 h until analytical thin layer chromatography indicated that the reaction was complete, the mixture was diluted with water (50 ml) and the SBO was extracted with dichloromethane (3¡Á20 ml), dried (MgSO4), filtered, evaporated under reduced pressure and recrystallized from aqueous methanol or ethanol.

With the rapid development of chemical substances, we look forward to future research findings about 701-16-6

Reference£º
Article; Ayrton, Stephen T.; Panova, Jekaterina; Michalik, Adam R.; Martin, William H.C.; Gallagher, Richard T.; Bowen, Richard D.; International Journal of Mass Spectrometry; vol. 345-347; (2013); p. 120 – 131;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

5-Chloro-6-hydroxybenzo[d]oxazol-2(3H)-one, cas is 1750-45-4, it is a common heterocyclic compound, the benzoxazole compound, its synthesis route is as follows.,1750-45-4

5-chloro-6-hydroxy-1,3-benzoxazol-2(3H)-one (0.93 g, 5 mmol) and imidazole (1.00 g, 15 mmol) were dissolved in dimethylformamide (10 mL) with stirring under inert atmosphere. Triisopropylsilylchloride (1.15 g, 6 mmol) was added and the resulting solution was stirred for 3 days. The reaction mixture was partitioned between water and heptane. The organic layer was washed with water and dried over magnesium sulphate, filtrated and concentrated, to give 1.45 g (85%) of the subtitled compound as a grey solid. APCI-MS: m/z 342 [MH+]

With the rapid development of chemical substances, we look forward to future research findings about 1750-45-4

Reference£º
Patent; ASTRAZENECA AB; WO2004/5295; (2004); 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

Benzo[d]oxazol-6-amine, cas is 177492-52-3, it is a common heterocyclic compound, the benzoxazole compound, its synthesis route is as follows.,177492-52-3

Benzooxazol-6-yl- (6-bromo-imidazo[1,2-a]pyrazin-8-yl)-amine [0133] A quantity of 0.13 g (1 mmole) OF BENZOOXAZOL-6-YLAMINE is treated with 0.27 g (1 mmole) OF 6, 8-DIBROMO-IMIDAZO [1, 2-a] pyrazine in acetonitrile with 3 eq OF K2CO3 AT REFLUX FOR 16 hrs. The reaction mixture is cooled partitioned between ethyl acetate and water, the organic extracts are dried over anhydrous MgSO4 and evaporated IN VACUO to afford BENZOOXAZOL-6-YL- (6-BROMO- imidazo [1, 2-a] pyrazin-8-yl)-amine.

With the rapid development of chemical substances, we look forward to future research findings about 177492-52-3

Reference£º
Patent; CELLULAR GENOMICS, INC.; WO2005/5429; (2005); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem