Heterocyclic Building Block-benzofuran

16859-59-9, 3-Hydroxyisobenzofuran-1(3H)-one is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 4: Alternative synthesis of Compound DE ED D(a) 2-Fluoro-5-[(E/Z)-(3-oxo-2-benzofuran- 1 (3H)-ylidene)methyl]benzonitrile (E) Sodium t-amylate (99.00 g, 0.854 mol) and 2-methyltetrahydrofuran (960 ml) were cooled to 2¡ãC under a nitrogen atmosphere. Diethyl phosphite (110 ml, 0.855 mol) was added dropwise maintaining the temperature at <5¡ãC. 2-Methyltetrahydrofuran (40 ml) was added as line wash. The reaction was stirred at 2¡ãC for 1 hour 40 minutes. A solution of 2-carboxybenzaldehyde (H)(80 g, 0.533 mol) in 2-methyltetrahydrofuran (200 ml) was added, maintaining the temperature at <7¡ãC throughout the addition. A line wash of 2-methyltetrahydrofuran (40 ml) was added. The reaction mixture was warmed to 200C and held at 200C for 20 minutes. Methanesulphonic acid (66 ml, 1.01 mol) was added over 1 hour and 10 minutes, followed by 2- methyltetrahydrofuran (40 ml). The reaction mixture was stirred at 20¡ãC over night. Methanesulphonic acid (7 ml, 0.101 mol) was added, followed by 2-methyltetrahydrofuran (7 ml) and the reaction stirred at 2O0C for a further 4 hours. Water (400 ml) was added at room temperature and the resulting biphasic mixture stirred at room temperature for 20 minutes. The lower aqueous layer was removed and a solution of potassium bicarbonate (53.50 g, 0.534 mol) in water (400 ml) was added to the organic layer. The biphasic mixture was stirred at room temperature for 20 minutes and then the lower aqueous solution was removed. The organic fraction was retained (solution of diethyl (3-oxo1 ,3-dihydro-2-benzofuran-1-yl)phosphonate). 16859-59-9, As the paragraph descriping shows that 16859-59-9 is playing an increasingly important role.

Reference£º
Patent; KUDOS PHARMACEUTICALS LIMITED; WO2008/47082; (2008); A2;,
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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) 6-Nitrophthalide (14.0 g; J A Houbion, J A Miles and J A Paton, Organic Preparations and Procedures International, 11 (1), 27, 1979) in solution in acetic acid was hydrogenated over a palladium on carbon catalyst to give 6-aminophthalide (12.0 g; W R Vaughan and S L Baird, J. Amer. Chem. Soc. 68, 1314, 1946).

The synthetic route of 610-93-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ICI Australia Limited; US4409017; (1983); A;,
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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

652-39-1, 3-fluoropurine (5.0 g, 30 mmol),3-aminopiperidine-2,6-dione hydrochloride (5.0 g, 30 mmol) andSodium acetate(3.7g, 45mmol)Add 100 mL of acetic acid. Heat to reflux for 12 h.Cool to room temperature and evaporate the acetic acid. Add 100 mL of water, extract 100 mL¡Á3 of ethyl acetate, and combine the organic phases with evaporated toluness.The compound (1a) was obtained in an amount of 7.5 g, and the yield was 90%.

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

Reference£º
Patent; Jilin University; Lu Haibin; Mu Xupeng; Bai Liting; Gao Zhuolin; Wang Ying; Zhao Linxuan; (23 pag.)CN109879877; (2019); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1914-60-9,2,3-Dihydrobenzofuran-2-carboxylic acid,as a common compound, the synthetic route is as follows.

General procedure: To a mixture of 7 (1 eq) and 1,1?-carbodiimidazole (1.2 eq) in anhydrous THF was stirred for 1h then substituted aniline (0.9 eq) was added at room temperature. After stirring for 14 h, solvent was evaporated then the mixture acidified with 6N HCl to pH 2. The mixture was extracted with EtOAc (3 ¡Á 20 mL). The combined extracts were dried over anhydrous Na2SO4and the solvent was evaporated. After evaporation, the residue was purified by column chromatography (EtOAc/hexane = 1:3 – 1:50).

1914-60-9, The synthetic route of 1914-60-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Choi, Minho; Jo, Hyeju; Park, Hyun-Jung; Sateesh Kumar, Arepalli; Lee, Joonkwang; Yun, Jieun; Kim, Youngsoo; Han, Sang-Bae; Jung, Jae-Kyung; Cho, Jungsook; Lee, Kiho; Kwak, Jae-Hwan; Lee, Heesoon; Bioorganic and Medicinal Chemistry Letters; vol. 25; 12; (2015); p. 2545 – 2549;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.54008-77-4,2-Bromobenzofuran,as a common compound, the synthetic route is as follows.

54008-77-4, General procedure: In a hot oven-dried Schlenk tube under N2 atmosphere were added Ph3Bi (0.25 mmol, 110 mg, 1.0 equiv), 2-bromobenzofuran (0.825 mmol, 163 mg, 3.3 equiv), Cs2CO3 (0.75 mmol, 244 mg, 3.0 equiv), Pd(OAc)2 (0.025 mmol, 5.6 mg, 0.1 equiv), PPh3 (0.1 mmol, 26 mg, 0.4 equiv), and NMP (3 mL) solvent. The resulting mixture was stirred in preheated oil bath at 90 C for 1 h. After the reaction is over, the mixture was cooled, quenched with dil HCl and extracted with ethyl acetate. The combined organic extract was washed with water, brine, and dried over MgSO4 and concentrated. The crude was subjected to silica gel column chromatography (230-400 mesh) using petroleum ether as the eluent to obtain the pure 2-phenylbenzofuran (2.1) as a white solid (140 mg, 96%). The product was characterized by spectroscopy and in comparison with the literature data.

54008-77-4 2-Bromobenzofuran 2776264, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Article; Rao, Maddali L.N.; Awasthi, Dheeraj K.; Talode, Jalindar B.; Tetrahedron Letters; vol. 53; 21; (2012); p. 2662 – 2666;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.64169-34-2,5-Bromoisobenzofuran-1(3H)-one,as a common compound, the synthetic route is as follows.

Step A: 5-(l,3-dioxolan-2-ylmethyl)-2-benzofuran-l(3H)-one A three-neck 5L round bottomed flask equipped with a stir bar, firestone valve, thermocouple, condenser and heating mantle was charged with tri-t-butyl phosphonium tetrafluoroborate (500 mg, 1.7 mmol), palladium (II) acetate (250 mg, 1.1 mmol) and 5-bromo-2-benzofuran-l(3H)-one (100 g, 470 mmol). DMF (1.9 L) was added to the flask, and the mixture was degassed three times by alternating vacuum and nitrogen purge. Commercially available bromo(l ,3-dioxolan- 2-ylmethyl)zinc solution (1.0 L, 520 mmol) was added via canula and the mixture was again degassed three times. The mixture was then heated at 85 C for 5 h. Analysis by HPLC-MS indicated the reaction was not complete. The mixture was stirred at 85 C for 5 more h. The mixture was then allowed to return to room temperature for overnight. 2-methyltetrahydrofuran (2.0 L) and brine were added, and the mixture was stirred for 5 min. The layers were separated and the aqueous layer was extracted again with 2-methyltetrahydrofuran. The organic layers were combined, washed three times with brine, dried over MgSC”4, filtered, and concentrated. The resulting residue was purified by flash chromatography (1.5 kg silica cartridge), eluting with 0->20% ethyl acetate in dichloromethane to afford 5-(l,3-dioxolan-2-ylmethyl)-2-benzofuran- l(3H)-one. MS: m/z 221 (M+l)+.

64169-34-2, As the paragraph descriping shows that 64169-34-2 is playing an increasingly important role.

Reference£º
Patent; MERCK SHARP & DOHME CORP.; WALSH, Shawn; PASTERNAK, Alexander; CATO, Brian; FINKE, Paul, E.; FRIE, Jessica; FU, Qinghong; KIM, Dooseop; PIO, Barbara; SHAHRIPOUR, Aurash; SHI, Zhi-Cai; TANG, Haifeng; WO2013/39802; (2013); A1;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13196-11-7,Benzofuran-6-ol,as a common compound, the synthetic route is as follows.

General procedure: To a mixture of 6 (1 mmol) and potassium carbonate (3 mmol) in anhydrous DMF (5 ml) was added corresponding benzo cyclic phenol (1.1 mmol). After the resulting mixture was heated at 90-110 C for 3-10 h, the reaction was cooled to room temperature and poured into water (15 ml). The mixture was extracted with ethyl acetate for three times, and the organic layers were combined, washed with saturated brine (20 ml x 2), dried over anhydrous magnesium sulfate and evaporated under reduced pressure. The residue was purified by flash column chromatography to yield the desired compound.

13196-11-7, 13196-11-7 Benzofuran-6-ol 128844, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Article; Zou, Qingan; Duan, Hongliang; Ning, Mengmeng; Liu, Jia; Feng, Ying; Zhang, Liming; Zhu, Junjie; Leng, Ying; Shen, Jianhua; European Journal of Medicinal Chemistry; vol. 82; (2014); p. 1 – 15;,
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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, General procedure: The catalytic reduction of nitro aromatics was conducted in a 25 mlTelfon-lined stainless steel autoclave with magnetic stirring. In a typicalprocess, 6 mmol nitroarene, and desired amounts of reducing agent andsolvents were introduced in the reactor. The autoclave was transferredinto a water bath at the set temperature with an accuracy of better than0.2 C for ?0.5 h. Then, 10 mg catalyst was added into the reactionmixture and started the reduction at a stirring rate of 450 rpm. After thereaction, the catalyst was rapidly separated by ltration. n-Decane(500 muL) as standard was added into the ltrate and was dried withanhydrous Na 2 SO 4 . The products were analyzed by gas chromato-graphy-mass spectrometry (GC-MS) (Shimadzu GCMS-QP2010 Plus)and GC (Varian CP-3800) with a capillary column (column VF-1 ms,15 m, 0.25 mm, 0.25 mum) and a ame ionization detector (FID).

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

Reference£º
Article; Huang, Haigen; Liang, Xiangcheng; Wang, Xueguang; Sheng, Yao; Chen, Chenju; Zou, Xiujing; Lu, Xionggang; Applied Catalysis A: General; vol. 559; (2018); p. 127 – 137;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.42933-43-7,2,3-Dihydrobenzofuran-5-amine,as a common compound, the synthetic route is as follows.

2,3-dihydro-benzofuran-5-amine (1A) (5.7 g, 42.20 mmol) was added to hydrochloric acid (10.2 mL, 12N) water (25 mL) was cooled to -5 ¡ã C to 0 ¡ã C, solution of sodium nitrite (3.2 g, 46.4 mmol) in water (20 mL) solution, after the addition was complete, 0 ¡ã C for 30 minutes to obtain a diazonium salt solution, standby; then sodium acetate (7.9 g , 97.1 mmol) in water (25 ml) with 1-chloro-1- (methylsulfonyl) propyl-2-one (7.2g, 42.2 mmol) in ethyl acetate (70 mL) mixed solution, maintaining 0 ¡ã C, the diazonium salt solution was slowly alternate dropwise added to the mixture, after the addition was complete, the reaction at room temperature for 4 hours. The reaction solution was extracted stratification, the organic phase dried over anhydrous sodium sulfate, and concentrated under reduced pressure, the residue was purified by silica gel column chromatography (ethyl acetate / petroleum ether (v / v) = l: 4) to give the title compound Nu-(2,3-dihydrobenzofuran-5-yl)-1-methylsulfonylmethanehydrazonoyl chloride (12B) as a yellow solid (1.3 g, yield 11.2percent).

42933-43-7, The synthetic route of 42933-43-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SICHUAN HAISCO PHARMACEUTICAL CO LTD; WEI, YONGGANG; QIU, GUANPENG; LEI, BAILIN; LU, YONGHUA; (120 pag.)CN104395312; (2016); B;,
Benzofuran – Wikipedia
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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.

Advanced intermediate VII (4.3 g; 0.01 mol) is stirred up in an aqueous solution of potassium carbonate (6.1 g; 0.044 mol in 20 ml of water) at the laboratory temperature. A toluene solution (20 ml) of intermediate VIII (2.41 g; 0.011 mol) is added to the mixture and the mixture is heated in an oil bath T=90 ¡ãC while being stirred for 3.5 h. After cooling the toluene layer is separated and the aqueous layer is extracted with toluene. The combined toluene extracts are shaken with water and the solvent is distilled off at a reduced pressure. The evaporation residue is dissolved in ethylmethylketone, and an equimolar amount of 48percent hydrobromic acid is added. The separated darifenacine hydrobromide is filtered off and dried.Yield: 86percent of theory.

127264-14-6, 127264-14-6 5-(2-Bromoethyl)-2,3-dihydrobenzofuran 21831160, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Patent; ZENTIVA, K.S.; WO2009/94957; (2009); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem