Day: September 14, 2020

132244-31-6, 5-Bromobenzo[d]oxazole is a benzoxazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a mixture of 5-bromobenzo[132244-31-6

132244-31-6 5-Bromobenzo[d]oxazole 21749504, abenzoxazole compound, is more and more widely used in various fields.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; DZIERBA, Carolyn Diane; BRONSON, Joanne J.; MACOR, John E.; DASGUPTA, Bireshwar; NARA, Susheel Jethanand; VRUDHULA, Vivekananda M.; PAN, Senliang; HARTZ, Richard A.; RAJAMANI, Ramkumar; (199 pag.)WO2016/22312; (2016); A1;,
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: A slurry of (2-chloro-4-(1-(3,4,5-trimethoxyphenyl)-lH-imidazol-4-ylamino)pyrrolo[1,2- f][1,2,4]triazin-7-yl)methanol (101b) (97 mg, 0.23 mmol), (S)-pyrrolidin-2-ylmethanol (171 mg, 1.69 mmol), di-tert-butyl(2′,4′,6′-triisopropylbiphenyl-2-yl)phosphine (di-t-Bu-XPhos, 14 mg, 0.034 mmol), Pd2(dba)3 (14 mg, 0.016 mmol), sodium tert-butoxide (162 mg, 1.69 mmol) in PhMe (5 mL) was degassed and placed in a sealed reactor. The reaction was heated at 100 ¡ãC for 48 hr, cooled to room temperature, quenched with saturated aqueous H4CI and extracted with ethyl acetate (3 x 20 mL). The organic layers were combined, washed with water, brine, dried, filtered and concentrated in vacuum to dryness. The residue obtained was purified by flash column chromatography (Silica gel 12 g, eluting with MeOH in DCM from 0 to 40percent) to afford (S)-(l-(7-(hydroxymethyl)-4-(l-(3,4,5-trimethoxyphenyl)-lH-imidazol-4- ylamino)pyrrolo[l,2-f][l,2,4]triazin-2-yl)pyrrolidin-2-yl)methanol (101c) (12 mg, 11 percent yield) as a white solid; MR (300 MHz, DMSO-^e) delta 10.47 (s, 1H, D20 exchangeable), 8.24 (d, J = 1.5 Hz, 1H), 7.97 (s, 1H), 7.10 (d, J= 4.4 Hz, 1H), 6.96 (s, 2H), 6.37 (d, J = 4.4 Hz, 1H), 4.67 (s, 2H), 4.32 – 4.09 (m, 1H), 3.88 (s, 6H), 3.79 – 3.70 (m, 1H), 3.68 (s, 3H), 3.67 – 3.52 (m, 1H), 3.53 – 3.20 (m, 2H), 2.14 – 1.75 (m, 4H); MS (ES+): 496.5 (M+l), 518.5 (M+Na); MS (ES-): 494.4 (M-l).

As the paragraph descriping shows that 4570-41-6 is playing an increasingly important role.

Reference£º
Patent; BIOCRYST PHARMACEUTICALS, INC.; KOTIAN, Pravin, L.; BABU, Yarlagadda, S.; KUMAR, V., Satish; ZHANG, Weihe; LU, Peng-Cheng; RAMAN, Krishnan; (747 pag.)WO2018/232094; (2018); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

22876-22-8, 5-Methylbenzo[d]oxazole-2(3H)-thione is a benzoxazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

INVENTIVE EXAMPLE 35 5-Methyl-2-(4-methyl-1-homopiperazinyl)benzoxazole 5-Methyl-2-mercaptobenzoxazole (200 mg) was dissolved in chloroform (20 ml), N-methylhomopiperazine (1.24 ml) was added dropwise to the solution and then the mixture was stirred with heating for 2 days. After evaporation of the solvent, the thus obtained mixture was purified by a silica gel column chromatography (methylene chloride_methanol=10:1) to obtain the title compound 5-methyl-2-(4-methyl-1-homopiperazinyl)benzoxazole (124 mg)., 22876-22-8

22876-22-8 5-Methylbenzo[d]oxazole-2(3H)-thione 710258, abenzoxazole compound, is more and more widely used in various fields.

Reference£º
Patent; Meiji Seika Kaisha, Ltd; Koichi Shudo; US6037342; (2000); 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.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, General procedure: Method E: A solution of the appropriate acid 3a (0.91 g, 5.1 mmol) inchloroform (20 mL) was cooled to 0 C with stirring. Thionyl chloride(1.75 mL, 24 mmol) was added dropwise, and the reaction mixture was heated at reflux for 5 h. After evaporation, the resulting crude acid chloride was dissolved in dichloromethane (50 mL),to 4 C, and added dropwise to a cooled mixture of 2-amino-4,6-dimethylpyridine(0.51 g, 4.8 mmol) and triethylamine (0.95 mL, 6.8 mmol) in dichloromethane (50 mL). The reaction mixture was then stirred at room temperature for 18 h. After evaporation of dichloromethane under vacuum, the residue was treated with water and the resulting precipitate filtered, washed with water, dried and recrystallised from 95% ethanol. Compound (4b) was synthesised in an identical fashion to (4a).

As the paragraph descriping shows that 54903-16-1 is playing an increasingly important role.

Reference£º
Article; Messaoud, Liacha; Wassila, Yahia; Khemissi, Seddiki; Yasmina, Adjeroud; Hanane, Chabane; Journal of Chemical Research; vol. 38; 6; (2014); p. 331 – 333;,
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.

5676-60-8 2-Methylbenzo[d]oxazol-6-amine 590539, abenzoxazole compound, is more and more widely used in various fields.

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

5-(benzyloxy)-4-chloro-6-p-tolylpyrimidine (50 mg, 0.161 mmol) was dissolved in PhMe, to this was added benzo[d]oxazol-6-amine (23.7 mg, 1.1 eq), Pd(dba)2 (4.6 mg, 0.05 eq), t-BuONa (31 mg, 2 eq), and (+/-)-BINAP (15 mg, 0.15 eq). The mixture was degassed and heated at 115C overnight. The mixture was cooled to room temperature, diluted with EtOAc and washed with H2O. Preparative TLC gave 17 mg of the title compound., 177492-52-3

The synthetic route of 177492-52-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SCHERING CORPORATION; CHELLIAH, Mariappan, V.; CHACKALAMANNIL, Samuel; GREENLEE, William, J.; EAGEN, Keith, A.; GUO, Zhuyan; CLASBY, Martin, C.; XIA, Yan; JAYNE, Charles, L.; DWYER, Michael; KEERTIKAR, Kartik, M.; CHAN, Tin-Yau; WANG, Li; WO2011/17296; (2011); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

701-16-6, 5-Fluoro-2-methylbenzo[d]oxazole is a benzoxazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

701-16-6, [0589] Compound 82: To a stirred solution of Comp-82b (0.1 g, 0.66 mmol) in mixture of THF (5 mL) and ffiuOH (1 mL) was added r-BuOK (0.2 g, 1.98 mmol) and the reaction mixture was stirred for 10 min. Comp-50c(0.1 g, 0.66 mmol) was added portion wise and the reaction mixture was stirred at room temperature for 16 h. Progress of the reaction was monitored by TLC and LCMS. After completion, the reaction mixture was quenched with H20 (5 mL) and extracted with EtOAc (10 mL X 2). The organic layer was washed with brine, dried over anhydrous Na2SO4 and concentrated under reduced pressure to get crude. The crude obtained was purified by prep HPLC to afford (E)-2-(2-(l-cyclopentyl-2,5- dimethyl-lH-pyrrol-3-yl)vinyl)-5-fluorobenzo[d]oxazole (82; 0.08 g, 40%) as white solid. (1026) [0590] HPLC Purity: 99.8% (1027) [0591] MS (ESI) m/e [M+H]+ Rt %: 325.2/2.47/99.4% (1028) [0592] 1H NMR (400 MHz, DMSO- d6) delta 1.62- 1.64 (m, 2 H), 1.82- 1.84 (m, 4 H), 1.98 – 2.08 (m, 2 H), 2.24 (s, 3 H), 2.36 (s, 3 H), 4.54 – 4.67 (m, 1 H), 6.26 (s, 1 H), 6.50 (d, J=15.65 Hz, 1 H), 7.10 – 7.19 (m, 1 H), 7.46 (dd, J=8.80, 2.45 Hz, 1 H), 7.62 – 7.64 (m, 1 H), 7.67 (d, J=15.65 Hz, 1 H).

As the paragraph descriping shows that 701-16-6 is playing an increasingly important role.

Reference£º
Patent; ALPINE ANDROSCIENCES, INC.; PATIL, Santhosh N.; SARMA, Bugga VNBS; (148 pag.)WO2019/152731; (2019); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

81900-93-8,81900-93-8, 4-Aminobenzo[d]oxazol-2(3H)-one is a benzoxazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 25: 1-(2-fluoro-4-(trifluoromethyl)benzyl)-3-(2,3-dihydro-2-oxobenzo[d]oxazol-4-yl)urea (scheme 1) Preparation of 1-(2-fluoro-4-(trifluoromethyl)benzyl)-3-(2,3-dihydro-2-oxobenzo[d]oxazol-4-yl)urea Commercially available 2-fluoro-4-trifluoromethylbenzylamine (0.5 ml, 3.7 mmol) was dissolved in 20ml of AcOEt and at 0C triphosgene (1.12 g, 3.7 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 drop wise to a solution in DMF (5 ml) of compound 1b (360 mg, 2.4 mmol) and the mixture was warmed at 80C for 8 hours. (TLC AcOEt). 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 100 mg of a white solid. Yield = 11% 1HNMR (DMSO, 400 MHz) delta 4.43 (2H, d, J = 6 Hz), 6.99 (3H, m), 7.05 (1H, m), 7.62 (3H, m), 8.53 (1H, bs), 10.98 (1H, bs); [M+1] 370.1 (C16H11F4N3O3 requires 369.27).

81900-93-8 4-Aminobenzo[d]oxazol-2(3H)-one 19982202, abenzoxazole compound, is more and more widely used in various fields.

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.72752-81-9,Methyl 2-mercaptobenzo[d]oxazole-6-carboxylate,as a common compound, the synthetic 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

The synthetic route of 72752-81-9 has been constantly updated, and we look forward to future research findings.

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

81900-93-8, 4-Aminobenzo[d]oxazol-2(3H)-one is a benzoxazole compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

81900-93-8, Preparation of 1-(4-(trifluoromethyl)-2-(piperidin-1-yl)benzyl)-3-(2,3-dihydro-2-oxobenzo[d]oxazol-4-yl)urea Amine 2c (350 mg, 1.33 mmol) was dissolved in 20 ml of AcOEt and at 0C triphosgene (395 mg, 1.33 mmol) was added to the solution. The mixture was warmed at 80C for 4 hours then evaporated and dissolved in 5ml of DMF. The solution of the isocyanate was added dropwise to a solution in DMF (10 ml) of compound 1b (100 mg, 0.66 mmol) and the mixture was warmed at 80C for 8 hours. (TLC AcOEt). 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 40 mg of a white solid. Yield = 14% 1HNMR (DMSO, 400 MHz) delta 1.55 (2H, m), 1.68 (4H, m), 2.85 (4H, m), 4.43 (2H, d, J = 5.6 Hz), 6.88 (1H, t), 6.98 (2H, m), 7.05 (1H, m), 7.31 (1H, s), 7.42 (1H, d), 7.52 (1H, d, J = 8 Hz), 8.52 (1H, s), 11.00 (1H, bs); [M+1] 435.3 (C21H21F3N4O3 requires 434.41).

The synthetic route of 81900-93-8 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