Heterocyclic Building Block-benzofuran

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.271-89-6,Benzofuran,as a common compound, the synthetic route is as follows.

General procedure: n-Butyllithium (1.67 M solution in hexane, 2.9 mL, 4.8 mmol) was added dropwise into a solution of 1,3-dimethoxybenzene (0.55 g, 4.0 mmol) in THF (5 mL) at 0 C and the mixture was stirred for 2 h at the same temperature. Then, DMF (0.34 mL, 4.4 mmol) was added to the mixture and the obtained mixture was stirred at 0 C. After 2 h at the same temperature, aq NH3 (8 mL, 120 mmol) and I2 (1.12 g, 4.4 mmol) were added and stirred for 2 h at rt. The reaction mixture was quenched with satd aq Na2SO3 (15 mL) and was extracted with Et2O (3¡Á20 mL). The organic layer was washed with brine and dried over Na2SO4 to provide 2,6-dimethoxybenzonitrile in over 80% purity. The product was purified by a short column chromatography on silica gel (Hexane/EtOAc=3:1) to give pure 2,6-dimethoxybenzonitrile in 91% yield as a colorless solid.

271-89-6 Benzofuran 9223, abenzofuran compound, is more and more widely used in various.

Reference£º
Article; Ushijima, Sousuke; Moriyama, Katsuhiko; Togo, Hideo; Tetrahedron; vol. 67; 5; (2011); p. 958 – 964;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.652-39-1,4-Fluoroisobenzofuran-1,3-dione,as a common compound, the synthetic route is as follows.

To methanol (175 mL) was added sodium hydride (3.36g, 60percent dispersion, 84.0 mmol) portionwise at ambient temperature under nitrogen. To the solution was added a solution of 3-fluorophthalic anhydride (5.56g, 33.5 mmol) in methanol (50 mL) dropwise under nitrogen at room temperature. The reaction was then worked-up as described for Example 56A to afford the title compound. The NMR data showed the product to be contaminated with 20percent of the 6-fluoro isomer. The material was used without further purification in the next step. 1H NMR (300 MHz, DMSO-J6) delta ppm 3.79 – 3.84 (two s, 3 H) 7.53 – 7.69 (m, 2 H) 7.76 (ddd, /=15.60, 7.29, 1.53 Hz, 1 H) 13.56 (s, 1 H); MS (+DCIZNH3) m/z 216.0 [M+NH4]+.

652-39-1 4-Fluoroisobenzofuran-1,3-dione 69551, abenzofuran compound, is more and more widely used in various.

Reference£º
Patent; ABBOTT LABORATORIES; AKRITOPOULOU-ZANZE, Irini; BRAJE, Wilfried; DJURIC, Stevan, W.; WILSON, Noel, S.; TURNER, Sean, C.; KRUGER, Albert, W.; RELO, Ana-Lucia; SHEKHAR, Shashank; WELCH, Dennie, S.; ZHAO, Hongyu; GANDARILLA, Jorge; GASIECKI, Alan, F.; LI, Huanqiu; THOMPSON, Christina, M.; ZHANG, Min; WO2010/135560; (2010); A1;,
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496-41-3, Benzofuran-2-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Oxalyl chloride (3.13 mL, 3.70 mmol) was added to a suspension of benzofuran-2- carboxylic acid (5.00 g, 3.08 mmol) in DCM (100 mL, anhydrous) and DMF (0.1 mL, 1.3 mmol) at r.t.. The mixture was stirred at r.t. for 1 h to give a colourless solution which was cooled to 0 C. N,O-Dimethylhydroxylamine hydrochloride (3.31 g, 3.39 mmol) and pyridine (7.5 mL, 9.27 mmol) were added sequentially and the mixture was stirred at r.t. for 18 h, then partitioned between EtOAc and sat. aq. NaHC03. Column chromatography (3 : 1 hexanes:EtOAc) gave 121 (6.32 g, 100%). 1H MR (CDC13) delta 7.69 (ddd, 7.9, 1.2, 0.7 Hz, 1H), 7.61 (ddd, J = 8.4, 1.7, 0.9 Hz, 1H), 7.51 (d, J = 1.0 Hz, 1H), 7.48 (ddd, J = 7.9, 7.2, 1.3 Hz, 1H), 7.30 (ddd, J = 7.5, 7.3, 0.9 Hz, 1H), 3.84 (s, 3H), 3.43 (s, 3H). Found: [M+H]=206.2. l-(Benzofuran-2-yl)-3-(dimethylamino ropan-l-one (122)

As the paragraph descriping shows that 496-41-3 is playing an increasingly important role.

Reference£º
Patent; THE GLOBAL ALLIANCE FOR TB DRUG DEVELOPMENT, INC.; UPTON, Anna, Marie; COOPER, Christopher, Blair; MARCEL, Koenraad, Jozel Lodewijk; GUILLEMONT, Jerome, Emile Goerges; VAN DEN BROECK, Walter Marcel, Mathilde; PALMER, Brian, Desmond; MA, Zhenkun; (186 pag.)WO2017/155909; (2017); A1;,
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496-41-3, Benzofuran-2-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: In a 20 or 40 mL reaction vial equipped with magnetic stir bar and Teflon-lined cap, a solution of the corresponding carboxylic acid (1.5 mmol, 3.0 eq) and DMAP (183.3 mg, 1.5 mmol, 3.0 eq) in anhydrous DMF (9.0 mL) was homogenized by stirring for 5-10min. EDCI¡¤HCl (287.6mg, 1.5mmol, 3.0 eq) was added, and the resulting mixture was homogenized by stirring for 5-10 min. The corresponding 1,3-indandione (0.5mmol, 1.0 eq) was added, and the resulting mixture was resealed and stirred for 12-72h, monitoring by LCMS. When complete, workup method A, B, or C was used to isolate the final products.

496-41-3 Benzofuran-2-carboxylic acid 10331, abenzofuran compound, is more and more widely used in various.

Reference£º
Article; Larsen, Brian J.; Rosano, Robert J.; Ford-Hutchinson, Thomas A.; Reitz, Allen B.; Wrobel, Jay E.; Tetrahedron; vol. 74; 22; (2018); p. 2762 – 2768;,
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Benzofuran | C8H6O – PubChem

641-70-3, 3-Nitrophthalic anhydride is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A round bottom flask was charged with a solution of glacial acetic acid (75 ml) and alpha-amino glutarimide hydrochloride (8.5 g). Sodium acetate anhydrous (4.5 g) was added lot-wise to the solution at 25 C. to 30 C. followed by addition of 3-nitro phthalic anhydride (log) at the same temperature. The reaction mixture was stirred at 118 C. for 18 hr. After the completion of reaction, the reaction mass was cooled to 60 C. and the solvent was distilled off under vacuum to get the residue. To the residue obtained, water (100 ml) was added; the mixture was stirred for 1 hr at 25 C. to 30 C. and the mass filtered. The wet cake obtained was slurried with water (100 ml*2), filtered and dried in an air tray dryer until the water content was less than 0.5% to afford 2-(2,6-dioxopiperidin-3-yl)-4-nitroisoindoline-1,3-dione (14 g). Yield: 89.7%, Purity: 98%.

As the paragraph descriping shows that 641-70-3 is playing an increasingly important role.

Reference£º
Patent; Apicore US LLC; Kovi, Ravishanker; Bobbili, Veerabhadra Rao; Kannapan, Jayaraman; (13 pag.)US2017/260157; (2017); 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.652-39-1,4-Fluoroisobenzofuran-1,3-dione,as a common compound, the synthetic route is as follows.

General procedure: To substituted phthalic anhydride (1.0 eq.) in 0.5 mL of DMSOwas added 4-aminoquinoline based diamines (1.0 eq.) in a microwavereaction vial. The vessel was sealed with a PTFE cap andheated to 160 ¡ãC for 2 min in a microwave reactor. After completionof the reaction as evident from TLC, the vessel contents werepoured in water (20 mL) and extracted with ethyl acetate(2 30 mL). The organic layers were combined, dried over anhydrous Na2SO4 and concentrated under reduced pressure toyield the crude product which was re-crystallized using absoluteethanol.

The synthetic route of 652-39-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Rani, Anu; Singh, Amandeep; Gut, Jiri; Rosenthal, Philip J.; Kumar, Vipan; European Journal of Medicinal Chemistry; vol. 143; (2018); p. 150 – 156;,
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

A mixture of 3-fluorophthalic anhydride (1 equiv.), 6-amino-1,2-thiazinan-3-one 1,1- dioxide (1 equiv.), and potassium acetate (2.5 equiv.) in acetic acid is stirred at 120 ¡ãC overnight. The dark mixture is cooled and filtered. The filter cake is dissolved in DCM and washed with saturated NaHCO3 and brine. The organic layer is dried (Na2SO4) and concentrated to provide 4-fluoro-2? -sulfonyl-thalidomide.

652-39-1 4-Fluoroisobenzofuran-1,3-dione 69551, abenzofuran compound, is more and more widely used in various.

Reference£º
Patent; C4 THERAPEUTICS, INC.; PHILLIPS, Andrew, J.; NASVESCHUK, Chris, G.; HENDERSON, James, A.; LIANG, Yanke; FITZGERALD, Mark, E.; MICHAEL, Ryan, E.; (790 pag.)WO2017/197056; (2017); A1;,
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Benzofuran | C8H6O – PubChem

641-70-3, 3-Nitrophthalic anhydride is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: A mixture of a cyclic anhydride 1 (1 mmol), guanidiniumchloride (2) (1 mmol), Et3N (2 mmol) and FeCl3 (10 mol%)in PEG-400 (0.5 mL) at 60C for aromatic derivatives andat 100C for aliphatic derivatives was stirred for an appropriatetime. The reaction progress was monitored by thinlayerchromatography. After the completion of the reaction,the reaction mixture was cooled to room temperature andthen was extracted with H2O and EtOAc. The organic layerwas dried over MgSO4 and then evaporated under reducedpressure. The residue was purified by column chromatographyon silica gel using n-hexane-EtOAc (7:3). The desired1H-isoindole-1,3(2H)-diones were obtained in 70-95%yields. Spectroscopy data for compounds 3 are in goodagreement with those previously reported.

641-70-3 3-Nitrophthalic anhydride 21631, abenzofuran compound, is more and more widely used in various.

Reference£º
Article; Ekhtiari, Zeinab; Havasi, Forugh; Nikpour, Farzad; Zeitschrift fur Naturforschung, B: Chemical Sciences; vol. 71; 9; (2016); p. 941 – 944;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.652-39-1,4-Fluoroisobenzofuran-1,3-dione,as a common compound, the synthetic route is as follows.

To a solution of 4-fluoroisobenzofuran-1,3-dione (661 mg, 3.98 mmol, CAS652-39-1), KOAc (1.21 g, 12.3 mmol) in HOAc (30 mL) was added 3-aminopiperidin-2-one (0.50 g, 4.38 mmol CAS1892-22-4). Then the mixture was stirred at 90 C. for 16 hours. On completion, the mixture was concentrated in vacuo to give a residue, which was then diluted with water 60 mL, and filtered to give the filter cake (0.60 g, 57% yield) as yellow solid. 1H NMR (400 MHz, DMSO-d6) delta 7.97-7.86 (m, 2H), 7.79-7.66 (m, 2H), 4.60 (dd, J=6.4, 12.0 Hz, 1H), 3.26-3.14 (m, 2H), 2.27-2.13 (m, 1H), 2.06-1.96 (m, 1H), 1.95-1.86 (m, 2H).

652-39-1 4-Fluoroisobenzofuran-1,3-dione 69551, abenzofuran compound, is more and more widely used in various.

Reference£º
Patent; Kymera Therapeutics, Inc.; Mainolfi, Nello; Ji, Nan; Kluge, Arthur F.; Weiss, Matthew M.; Zhang, Yi; (1443 pag.)US2019/192668; (2019); 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.496-41-3,Benzofuran-2-carboxylic acid,as a common compound, the synthetic route is as follows.

4.1.2.2. 1-(Benzofuran-2-yl)-3-(dimethylamino)propan-1-one (classD-2). Oxalyl chloride (3.13 mL, 3.70 mmol) was added to a suspensionof benzofuran-2-carboxylic acid (5.00 g, 3.08 mmol) in DCM(100 mL, anhydrous) and DMF (0.1 mL, 1.3 mmol) at 20 C. Themixture was stirred at 20 C for 1 h to give a colourless solutionwhich was cooled to 0 C. N,O-Dimethylhydroxylamine hydrochloride(3.31 g, 3.39 mmol) and pyridine (7.5 mL, 9.27 mmol) wereadded sequentially and the mixture was stirred at 20 C for 18 h,then partitioned between EtOAc and sat. aq. NaHCO3. Column chromatography(3:1 hexanes:EtOAc) gave N-methoxy-N-methylbenzofuran-2-carboxamide (6.32 g, 100%). 1H NMR (CDCl3) d 7.69(ddd, 7.9, 1.2, 0.7 Hz, 1H), 7.61 (ddd, J = 8.4, 1.7, 0.9 Hz, 1H),7.51 (d, J = 1.0 Hz, 1H), 7.48 (ddd, J = 7.9, 7.2, 1.3 Hz, 1H), 7.30(ddd, J = 7.5, 7.3, 0.9 Hz, 1H), 3.84 (s, 3H), 3.43 (s, 3H). Found:[M+H] = 206.2.

The synthetic route of 496-41-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Sutherland, Hamish S.; Tong, Amy S.T.; Choi, Peter J.; Conole, Daniel; Blaser, Adrian; Franzblau, Scott G.; Cooper, Christopher B.; Upton, Anna M.; Lotlikar, Manisha U.; Denny, William A.; Palmer, Brian D.; Bioorganic and Medicinal Chemistry; vol. 26; 8; (2018); p. 1797 – 1809;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem