Month: October 2020

6940-49-4, 3-Bromophthalide is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(1) Preparation of N,N,N-triethyl-3-oxo-1,3-dihydro-1-isobenzofuranylammonium bromide STR11 A mixture of 8.52 g (40 mmol) of 3-bromo-1,3-dihydro-1-isobenzofuranone 1 and 27.87 ml (200 mmol) of triethylamine in 85 ml of tetrahydrofuran is allowed to react at room temperature for 96 hours, and the precipitating crystals are filtered and washed with dichloromethane to give 11.04 g of the titled compound 2. (Yield: 88%) m.p. 173-174 C. NMR: deltad6 DMSO 1.25 (t, J=8.0 Hz, 9H), 3.58 (q, J=8.0 Hz, 6H), 7.16 (s, 1H), 7.80-8.23 (m, 4H). Elemental analysis (%) Calcd: C, 53.51; H, 6.42; N, 4.46 (for C14 H20 NO2 Br). Found: C, 53.07; H, 6.42; N, 4.52.

6940-49-4, The synthetic route of 6940-49-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Shionogi & Co., Ltd.; US4605738; (1986); A;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.21535-97-7,3-Methylbenzofuran,as a common compound, the synthetic route is as follows.

Compound E-3 (16 g, 121 mmol) was dissolved in 1,4-dioxane solution (100 mL), and then add selenium dioxide (17.5g, 157mmol), then, the mixture was stirred and refluxed for 16 hours. The reaction was cooled to room temperature, and the mixture was diluted with ethyl acetate /hexane (2:1, 100 mL). After stirring for 10 min, the insoluble material was removed by filtration and washed with ethyl acetate. The combined filtrates were concentrated under reduced pressure and purified by silica gel column chromatographyThe product was obtained as a yellow solid 7.3 g, yield 41%, 21535-97-7

The synthetic route of 21535-97-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Sichuan University; Li Guobo; Wu Yong; Wang Yaoling; Liu Sha; Yu Zhujun; Yan Yuhang; Huang Mengyi; (39 pag.)CN110156820; (2019); A;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.189035-22-1,6-Bromo-2,3-dihydrobenzofuran,as a common compound, the synthetic route is as follows.

The title compound was prepared according to procedures reported in the literature and known by persons skill in the art, using 6-bromo-2,3-dihydro-1-benzofuran (1 g, 5.03 mmol) as starting material. In a preferred method, 6-bromo-2,3-dihydro-1-benzofuran (1 g, 5.03 mmol) in toluene (10 mL) was degassed for 30 min. To this solution, 1-ethoxyvinyl tributyltin (2.012 g, 5.53 mmol) and bis(triphenylphosphine)palladium dichloride (0.35 g, 0.50 mmol) were added at rt and stirred for 16 hours at 90 C. The reaction mixture was cooled to rt and filtered through celite. After evaporation of the solvent, 6 N HCl solution in water (10 mL) was added and the mixture was stirred for 1 hour at rt. It was concentrated and neutralized with sat. NaHCO3. The desired product was extracted with DCM (50 mL), dried over Na2SO4 and concentrated. The crude product was purified by flash chromatography to give the title compound. Yield: 73.7% (0.6 g, pale yellow solid). 1H NMR (400 MHz, DMSO-d6): delta 7.48 (d, J = 7.64 Hz, 1H), 7.37-7.35 (d, J = 7.68 Hz, 1H), 7.26 (s, 1H), 4.58 (t, J = 8.76 Hz, 2H), 3.24 (t, J = 8.76 Hz, 2H), 2.53 (s, 3H). LCMS: (Method A) 163.2 (M+H), Rt. 3.01 min, 97.60% (Max)., 189035-22-1

189035-22-1 6-Bromo-2,3-dihydrobenzofuran 11252616, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Patent; ASCENEURON S. A.; QUATTROPANI, Anna; KULKARNI, Santosh S.; GIRI, Awadut Gajendra; KOEK, Johannes Nicolaas; (64 pag.)WO2017/144635; (2017); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

652-39-1, 4-Fluoroisobenzofuran-1,3-dione is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

652-39-1, Step 1: Synthesis of 2-(2,6-dioxopiperidin-3-yl)-4-fluoroisoindoline-1,3-dione A solution of 4-fluoroisobenzofuran-1,3-dione (200 mg, 1.20 mmol, 1 equiv) in AcOH (4.0 mL, 0.3 M) was added 2,6-dioxopiperidin-3-amine hydrochloride (218 mg, 1.32 mmol, 1.1 equiv) and potassium acetate (366 mg, 3.73 mmol, 3.1 equiv). The reaction mixture was heated to 90 oC overnight, whereupon it was diluted with water to 20 mL and cooled on ice for 30 min. The resulting slurry was filtered, and the black solid was purified by flash column chromatography on silica gel (2% MeOH in CH2Cl2, Rf = 0.3) to afford the title compound as a white solid (288 mg, 86%). 1H NMR (500 MHz, DMSO-d6) delta 11.15 (s, 1H), 7.96 (ddd, J = 8.3, 7.3, 4.5 Hz, 1H), 7.82 – 7.71 (m, 2H), 5.17 (dd, J = 13.0, 5.4 Hz, 1H), 2.90 (ddd, J = 17.1, 13.9, 5.4 Hz, 1H), 2.65- 2.47 (m, 2H), 2.10- 2.04 (m, 1H), MS (ESI) cald for C13H10FN2O4 [M+H]+ 277.06, found 277.25.

As the paragraph descriping shows that 652-39-1 is playing an increasingly important role.

Reference£º
Patent; DANA-FARBER CANCER INSTITUTE, INC.; BUCKLEY, Dennis; WINTER, Georg; PHILLIPS, Andrews, J.; HEFFERNAN, Timothy, P.; BRADNER, James; ROBERTS, Justin; BEHNAM, Nabet; (544 pag.)WO2018/148443; (2018); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.610-93-5,6-Nitroisobenzofuran-1(3H)-one,as a common compound, the synthetic route is as follows.

610-93-5, A mixture of compounds 12 (10 mmol) and 10% (mass fraction) Pd/C (0.20 g) in MeOH (20 mL) was subjected to standard hydrogenolysis condition at atmospheric pressure (balloon) and room temperature. The progress of the reaction was monitored by TLC. After completion of the reactions, the reaction mixture was filtered off and the filtrate was evaporated on a rotary evaporator to afford the crude products 13, which were used directly in the next step without further purification. Yield: 87%, Mp: 186-187 C. 1H-NMR (CDCl3, 600 MHz), d: 7.28(s, 1H, ArH), 7.11-7.07(m, 1H, ArH), 7.05(dd, J = 8.1Hz, 2.1Hz, 1H, ArH), 5.25(s, 2H), 3.95(s, 2H, NH2). 5110 X. Hu et al. 123

610-93-5 6-Nitroisobenzofuran-1(3H)-one 223584, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Article; Hu, Xia-min; Cui, Zhi-wen; Dong, Wei; Zhu, Yue; Gao, Cheng-zhi; Xu, Shi-qiang; Yuan, Qiong; Yu, Zhi-jun; Min, Zhen-li; Research on Chemical Intermediates; vol. 44; 9; (2018); p. 5107 – 5122;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

4265-25-2, 2-Methylbenzofuran is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,4265-25-2

Compound 5c was prepared by an analogous method similar to that used for 5aand obtained as a light yellow liquid in 52% yield. 1H NMR (400 MHz, CDCl3, TMS): delta2.49 (s, 3H, -CH3), 7.25-7.34(m, 3H, phenyl-H), 7.40-7.47 (m, 1H, phenyl-H)

As the paragraph descriping shows that 4265-25-2 is playing an increasingly important role.

Reference£º
Article; Wang, Renjie; Pu, Shouzhi; Liu, Gang; Cui, Shiqiang; Li, Hui; Tetrahedron Letters; vol. 54; 39; (2013); p. 5307 – 5310;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

13414-56-7, 2,3-Dihydrobenzofuran-7-amine is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

At 0 deg.] C, the solid 2,3-dihydrobenzofuran-7-amine (5 g, 37 mmol) was dissolved in DMF (60 ml) in added portionwise NBS (7.2 g, 41 mmol), stirred for 10 minutes after natural warming stirred at 20 ~ 30 3 hours.Most of the solvent was distilled off under reduced pressure, and the residue was purified by silica gel chromatography to give the title compound through column (yellow solid, 6 g, 76% yield).LCMS (ESI) m / z: 214,216 (M + 1, M + 3).

13414-56-7, 13414-56-7 2,3-Dihydrobenzofuran-7-amine 12805950, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Patent; Shanghai Biological Technology Co., Ltd. opened Mai; yao, li; (18 pag.)CN105481841; (2016); A;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.127264-14-6,5-(2-Bromoethyl)-2,3-dihydrobenzofuran,as a common compound, the synthetic route is as follows.

Example 9:Preparation of darifenacin hydrochloride:To 3-(S)-(+)-(l-carbamoyl-l,l-diphenyl methyl) pyrrolidine tartrate (100 grams) taken in water (500 ml), a solution of aqueous sodium hydroxide was added till the pH reached 14. The reaction mixture was stirred for 20 min at 25-300C, sodium chloride(150 grams) was added to it and stirred further for 20min. The reaction mixture was heated to 55-600C and extracted with toluene. The toluene layer was washed with 5percent sodium chloride solution and the solvent distilled off under reduced pressure. The residue was dissolved in acetonitrile, 5-(2-bromoethyl) 2,3-dihydrobenzofuran (66 grams dissolved in 800 ml acetonitrile) and potassium hydroxide (13 grams) was added to it.The reaction mixture was heated to 40-500C and stirred for 18 hrs. The reaction mixture was cooled to 25-30¡ãC and filtered. The acetonitrile solvent was distilled off under reduced pressure. The residue was dissolved in acetone, cooled to 0-5 ¡ãC and hydrochloric acid (36 ml) was added to it. The temperature was raised to 25-30¡ãC and stirred for 12 hrs. The reaction mixture was cooled to 0-5¡ã C, the solid obtained was filtered, washed with acetone and dried. It was purified using methanol and acetone to provide the title compound as a white solid. Yield: 75 grams Example 11:Preparation of darifenacin hydrobromide:To 3 -(S)-(+)-(l -carbamoyl -1,1 diphenyl methyl) pyrrolidine tartrate (100 grams) taken in water (500 ml), a solution of aqueous sodium hydroxide was added till the pH reached 14. The reaction mixture was stirred for 20 min at 25-30¡ãC and sodium chloride(150 grams) was added to it and stirred for 20min. The reaction mixture was heated to55-6O0C and extracted with toluene. The toluene layer was washed with 5percent sodium chloride solution and the solvent distilled off under reduced pressure. The residue was dissolved in acetonitrile, 5-(2-bromoethyl)-2,3-dihydrobenzofuran (66 grams dissolved in 800 ml acetonitrile) and potassium hydroxide (13 grams) was added to it. The reaction mixture was heated to 40-50¡ãC and stirred for 18 hrs. The reaction mixture was cooled to 25-30¡ãC and filtered. The acetonitrile solvent was distilled off under reduced pressure. The residue was dissolved in acetone, cooled to 0-5¡ãC and hydrobromic acid (36 ml) was added to it. The temperature was raised to 25-30¡ãC and stirred for 12 hrs. The reaction mixture was cooled to 0-5¡ã C, the solid obtained was filtered, washed with acetone and dried. It was purified using methanol and acetone to provide the title compound as a white solid.Yield: 75 gramsSOR: +45 (C=I, dichloromethane)

127264-14-6, The synthetic route of 127264-14-6 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SATYANARAYANA REDDY, Manne; THIRUMALAI RAJAN, Srinivasan; VENKATESH, Mummadi; WO2008/126106; (2008); A2;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

652-40-4, 4,7-Difluoroisobenzofuran-1,3-dione is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

652-40-4, (3) Methyl 3-(4,7-difluoro-1,3-dioxo-1,3-dihydro-isoindol-2-yl)-2-(2-methyl-[1,3]dioxolan-2-yl)propionate Methyl 3-(4,7-difluoro-1,3-dioxo-1,3-dihydro-isoindol-2-yl)-2-(2-methyl-[1,3]dioxolan-2-yl)propionate was prepared (0.27 g, 31percent) in the same manner as described in the above example 5. (1) from methyl 3-amino-2-(2-methyl-[1,3]dioxolan-2-yl)propionate (0.47 g, 2.47 mmol) and 3,6-difluorophthalic anhydride (0.50 g, 2.72 mmol), and the obtained product was identified with the following NMR data. 1H NMR (CDCl3, 300 MHz) delta 7.31 (t, 2H, ph, J=5.3 Hz), 3.95 (m, 6H, acetal H, -CHCH2NPht), 3.64 (s, 3H -CO2CH3), 3.20 (m, 1H, -CHCH2NPht), 1.42 (s, 3H, CH3) 3C NMR (CDCl3, 300 MHz) delta 171.9, 163.9, 155.8, 152.2, 125.5, 121.1, 120.6, 120.1, 108.9, 65.4, 60.9, 53.8, 51.7, 37.2, 22.0, 14.5

As the paragraph descriping shows that 652-40-4 is playing an increasingly important role.

Reference£º
Patent; Korea Institute of Science and Technology; US2003/139464; (2003); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.16859-59-9,3-Hydroxyisobenzofuran-1(3H)-one,as a common compound, the synthetic route is as follows.

General procedure: 2-Formylbenzoic acid (1a; 1.0 equiv) was heated at reflux in SOCl2 (5?10 equiv) for 4 h at 100 ¡ãC. The remaining SOCl2 was removed in vacu-um and the obtained solid was dissolved in CH2Cl2 (10 mL). The mix-ture was cooled to 0 ¡ãC and the desired primary amine (2.0 equiv)was slowly added. The solution was stirred for 24 h at r.t. then thereaction mixture was diluted with EtOAc (70 mL), washed with citricacid (0.5 M), sat. aq Na2CO3 solution, and brine. The organic layer wasdried over MgSO4 and the solvent was removed under reduced pres-sure. The obtained products were used without further purification., 16859-59-9

The synthetic route of 16859-59-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Niedek, Dominik; Schuler, Soeren M.M.; Eschmann, Christian; Wende, Raffael C.; Seitz, Alexander; Keul, Felix; Schreiner, Peter R.; Synthesis; vol. 49; 2; (2017); p. 371 – 382;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem