Heterocyclic Building Block-benzofuran

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;,
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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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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;,
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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;,
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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;,
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Benzofuran | C8H6O – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.102308-43-0,4-Bromo-2-benzofuran-1[3H]-one,as a common compound, the synthetic route is as follows.

To a stirring solution of 3,4-dimethoxy-2-(methoxymethyl)phenylboronic acid(compound 301)(2.3 g, 10.79 mmol) in dimethylformamide (25 mL) under nitrogen atmosphere, were added cesium carbonate (10.52 g, 32.31 mmol),tetrakis(triphenylphosphine)palladium(0) (623 mg, 0.539 mmol) and 4- bromoisobenzofuran-l(3H)-one (5.2 g, 21.5 mmol) and the resultant reaction mixture was heated to 80 C for 3 h. The reaction mixture was filtered off and the filtrate was extracted with ethyl acetate (3 x). The combined ethyl acetate layer was washed with brine and dried over anhydrous sodium sulphate and concentrated under reduced pressure. Purification by column chromatography (silica gel, 0-30% ethyl acetate in pet ether) afforded 4-(3,4-dimethoxy-2-methoxymethoxy-phenyl)-3H-isobenzofuran-l-one as a solid.

102308-43-0 4-Bromo-2-benzofuran-1[3H]-one 11593715, abenzofuran compound, is more and more widely used in various.

Reference£º
Patent; LEO PHARMA A/S; NIELSEN, Simon Feldbaek; HORNEMAN, Anne Marie; LAU, Jesper Faergemann; LARSEN, Jens Christian H¡ãjland; WO2011/134468; (2011); A1;,
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4265-16-1, Benzo[b]furan-2-carboxaldehyde is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a solution of aldehyde 1 (1 equiv.) in tetrahydrofuran (THF) was slowly added 1.0 M allyl magnesium bromide (2 equiv.) at 0 oC. Some of the aldehydes 1f-1m, 1w, and 1x were treated with the solution of zinc and allyl bromide instead of allyl magnesium bromide because allyl magnesium bromide did not work properly. The reaction mixture was warmed to room temperature and stirred for 2-12 h. Saturated NH4Cl aqueous solution was added to the mixture and it was poured into ethyl acetate and extracted with ethyl acetate 2 times. The combined organic layers were washed with brine, dried with Na2SO4, filtered, and concentrated. The residue was purified by silica gel column chromatography (Hexane/Ethyl acetate) to give compounds 2 (26-99% of yield).

4265-16-1 Benzo[b]furan-2-carboxaldehyde 61341, abenzofuran compound, is more and more widely used in various.

Reference£º
Article; Lee, Sun-Mi; Lee, Won-Gil; Kim, Young-Chul; Ko, Hyojin; Bioorganic and Medicinal Chemistry Letters; vol. 21; 19; (2011); p. 5726 – 5729;,
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Benzofuran | C8H6O – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.69999-16-2,2,3-Dihydrobenzofuranyl-5-acetic acid,as a common compound, the synthetic route is as follows.

EXAMPLE 6 Obtaining 2-(2,3-dihydrobenzofuran-5-yl)-acetamide [Show Image] 5 ml of DMF and a solution of 45 ml (0.617 moles) of thionyl chloride in 100 ml of acetonitrile were added consecutively to a solution of 100 g (0.560 moles) of (2,3-dihydrobenzofuran-5-yl)-acetic acid in 900 ml of acetonitrile. The reaction mixture was maintained at 45C for 4 hours. Once the reaction was finished, the obtained solution was cooled at 15C and was slowly added during approximately one hour to a mixture consisting of 800 ml of 25% NH3 aqueous solution and 400 ml of acetonitrile cooled at 5C. Once the reaction mixture was added, it was maintained at room temperature for 4 hours. Then 800 ml of water were added and it was stirred for 30 minutes; the obtained phases were separated and the aqueous phase was extracted with 2x 100 ml of acetonitrile. The combined extracts were concentrated under vacuum to a final volume of 500 ml. The obtained suspension was maintained under stirring at 5C for 30 minutes and the solid was isolated by filtration, obtaining 96.5 g (97% yield) of a white solid having the following spectroscopic properties: 1H NMR (400 MHz, DMSO): 3.09 (2H, t, J=8Hz), 3.26 (2H, s), 4.45 (2H, t, J=8Hz), 6.64 (1H, d, J=8Hz), 6.81 (1H, s), 6.93 (1H, d, J=8Hz), 7.09 (1H, s), 7.34 (1H, s) ppm. 13C NMR (100 MHz, DMSO): 29.12 (CH2), 41.69 (CH2), 70.79 (CH2), 108.39 (CH), 125.7 (CH), 127.09 (C), 128.21 (C), 128.33 (CH), 158.30 (C), 172.89 (C) ppm. LRMS (electrospray, positive ion): m/z [M++Na+] 199.8

As the paragraph descriping shows that 69999-16-2 is playing an increasingly important role.

Reference£º
Patent; Ragactives, S.L.; EP2236509; (2010); A1;,
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610-93-5, 6-Nitroisobenzofuran-1(3H)-one is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a screw top vial (5 mL) under N2 containing freshly distilled toluene (0.6 mL) were successively added an aromatic nitro compound (0.60 mmol), InI3 (14.9 mg, 0.030 mmol), and TMDS (318 muL, 1.80 mmol). After the vial was sealed with a cap that contained a PTFE septum, the mixture was stirred at 60 C (bath temperature), and monitored via TLC analysis. Sat. aq NaHCO3 solution (5 mL) was added to the resultant mixture, which was then extracted with EtOAc (3 ¡Á 6 mL). The combined organic phases were dried over anhydrous Na2SO4, filtered, and concentrated under reduced pressure. The crude product was purified by silica gel column chromatography (n-hexane-EtOAc, 9:1 to 4:1) to afford the corresponding aniline derivative.

As the paragraph descriping shows that 610-93-5 is playing an increasingly important role.

Reference£º
Article; Sakai, Norio; Asama, Shun; Konakahara, Takeo; Ogiwara, Yohei; Synthesis; vol. 47; 20; (2015); p. 3179 – 3185;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.569-31-3,6,7-Dimethoxy-3H-1-isobenzofuranone,as a common compound, the synthetic route is as follows.

To a solution of compound 31a (6.31 g, 32.5 mmol) in acetonitrile (60 mL) was added NCS (4.77 g, 35.7 mmol). After stirring at 60 C. for 1 hour, the insoluble matter was collected by filtration, whereby Compound 31b was obtained.

569-31-3 6,7-Dimethoxy-3H-1-isobenzofuranone 68437, abenzofuran compound, is more and more widely used in various.

Reference£º
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; GLAXO GROUP LIMITED; YAMAWAKI, KENJI; YOKOO, KATSUKI; SATO, JUN; KUSANO, HIROKI; AOKI, TOSHIAKI; LIAO, XIANG MIN; PEARSON, NEIL DAVID; PENDRAK, ISRAIL; THALGI, REEMA; (373 pag.)JP6377570; (2018); B2;,
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Benzofuran | C8H6O – PubChem