Heterocyclic Building Block-benzofuran

10242-12-3, 5-Nitrobenzofuran-2-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Under nitrogen protection conditions, 5 mL of anhydrous dichloromethane was addedNitrobenzofuran-2-carboxylic acid (23 mg, 0.11 mmol)After stirring at room temperature, HOBt (18 mg, 0.13 mmol) was added,After stirring for 10 minutes, EDC ¡¤ HCl (25 mg,0.13 mmol) followed by the addition of compound III-8-a of Example 6(50 mg, 0.17 mmol) and DIPEA (0.04 mL, 0.22 mmol)TLC after 15 hours showed complete reaction,The reaction solution was washed with 5% NaHCO3 solution, 10% citric acid solution,5% NaHCO3 solution and saturated brine,Adding to the organic phase anhydrous sodium sulfate drying, drying and filtering,The solvent was removed using a rotary evaporator and the product was added directly to 5 mL of methanol,After stirring at room temperature, 2-methylpropylboronic acid (22 mg, 0.22 mmol) was added5 mL of n-hexane, followed by the addition of 1 M HCl solution (0.33 mL, 0.33 mmol)After 5 hours, the TLC assay showed complete reaction, the reaction solution was allowed to stand,The lower layer was washed with n-hexane, dried over anhydrous sodium sulfate,Drying after filtration, the use of rotary evaporator in addition to solvent,Column chromatography (dichloromethane: methanol = 60: 1) gave 17 mg of a yellow solid,Yield 48%, 10242-12-3

The synthetic route of 10242-12-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Fudan University; Shao Liming; Xu Yulong; Chen Yiyi; Li Wei; Xie Qiong; (36 pag.)CN107151255; (2017); A;,
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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.59434-19-4,4-Aminophthalide,as a common compound, the synthetic route is as follows.,59434-19-4

To a solution of 4-aminoisobenzofuran-1(3H)-one (1 g, 6.7 mmol) and 1-(4-fluorophenyl)ethanone (1.4 g, 10.1 mmol) in toluene (35 mL) was added anhydrous magnesium sulfate (8.8 g, 73.7 mmol) and acetic acid (0.2 mL) at room temperature under N2. The reaction mixture was then stirred at 120 C. for 36 hr. The reaction mixture was cooled to 90 C. and filtered. After filter cake was washed with acetonitrile, the filtrates were combined and evaporated to dryness to obtain yellow solid, which was washed by petroleum ether to obtain the title compound as a white solid (1.58 g, yield 88%). LC-MS (ESI) m/z: 270(M+1)+H-NMR (400 MHz, CDCl3) delta (ppm): 2.30 (s, 3H), 5.16 (s, 2H), 7.00-7.02 (d, J=7.6 Hz, 1H), 7.13-7.18 (m, 2H), 7.51-7.56 (t, J=7.6 Hz, 1H), 7.66-7.69 (d, J=7.6 Hz, 1H), 7.99-8.03 (m, 2H).

As the paragraph descriping shows that 59434-19-4 is playing an increasingly important role.

Reference£º
Patent; LEAD THERAPEUTICS, INC.; US2010/35883; (2010); A1;,
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Benzofuran | C8H6O – PubChem

496-16-2, 2,3-Dihydrobenzo[b]furan is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

56 g (0.42 mol) of aluminum trichloride is added to 280 g of methylene chloride,Cool to 0¡ãC,Temperature drop below 10¡ãC45 g (0.33 mol) monoethyl oxalyl chloride,After the drop, the heat preservation reaction is 1hr,36 g (0.30 mol) of 2,3-dihydrobenzofuran (Compound 3) was added dropwise below 10¡ã C., and the reaction was allowed to proceed overnight at room temperature.After confirming the reaction,The reaction solution was poured into 300 g of ice water,Stirring liquid,Extract with dichloromethane (100g x 2)Combine the organic phase,Wash once with 200 g of saturated aqueous sodium bicarbonate,filter,The filtrate was dried over anhydrous sodium sulfate.Filtered,Concentrate to give about 73 g of oil (theoretical amount: 65.98 g).

496-16-2, As the paragraph descriping shows that 496-16-2 is playing an increasingly important role.

Reference£º
Patent; Inner Mongolia Jingdong Pharmaceutical Co., Ltd.; Guo Rongyao; Wang Xiaofeng; (9 pag.)CN107721954; (2018); A;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.7169-34-8,Benzofuran-3(2H)-one,as a common compound, the synthetic route is as follows.,7169-34-8

General procedure: A mixture of benzofuran-3(2H)-one (2.0 mmol), benzaldehyde (2.2mmol) and water (5 mL) was stirred at reflux temperature for 6-10 h. Completion of the reaction was checked on TLC. Then the mixture was allowed to rt and stirred for 1 h. The precipitated solids were filtered, washedwith water (2 ¡Á 5 mL) and dried to give the product. (Z)-2-Benzylidenebenzofuran-3(2H)-one (4a). Pale yellow color solid (380 mg, 86%), mp 102-104 C (lit.23 mp110-111 C). 1H NMR (CDCl3): 7.93 (2H, d, J 6.8 Hz), 7.82 (1H, d, J 7.6 Hz), 7.66 (1H, t, J 8.2 Hz), 7.38-7.48 (3H,m), 7.34 (1H, d, J 8.0 Hz), 7.22 (1H, t, J 7.4 Hz), 6.90 (1H, s); 13C NMR (CDCl3): 184.7, 166.2, 146.9, 136.8, 132.4,131.5, 129.9, 128.9, 124.7, 123.5, 121.7, 113.0, 112.9; LC-MS (positive ion mode): m/z 223 (M+H)+.

As the paragraph descriping shows that 7169-34-8 is playing an increasingly important role.

Reference£º
Article; Venkateswarlu, Somepalli; Murty, Gandrotu Narasimha; Satyanarayana, Meka; Arkivoc; vol. 2017; 4; (2017); p. 303 – 314;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.15832-09-4,6-Methoxy-3(2H)-benzofuranone,as a common compound, the synthetic route is as follows.

General procedure: To a solution of compound 3a or 3b (2.0 mmol) in methanol (20 mL) was added successively anaqueous 50% potassium hydroxide (3 mL) and benzaldehyde derivatives 4 (3.0 mmol). The mixture was heated at 60 C and then solvent was evaporated. The residue was diluted in water and extracted with ethyl acetate. The organic layer was dried over anhydrous MgSO4 and filtered. The filtrate was concentrated and purified by silica gel column chromatography to give aurones., 15832-09-4

The synthetic route of 15832-09-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Shin, Seo Young; Shin, Min Cheol; Shin, Ji-Sun; Lee, Kyung-Tae; Lee, Yong Sup; Bioorganic and Medicinal Chemistry Letters; vol. 21; 15; (2011); p. 4520 – 4523;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.10242-10-1,5-Chlorobenzofuran-2-carboxylic acid,as a common compound, the synthetic route is as follows.

To a solution of N-(l-aminopiperidin-4-yl)-2-(4-chloro-3-fluorophenoxy) acetamide (0.100 g, 0.33 mmol, 1.0 equiv) in DMF (5 mL) was added 5-chlorobenzofuran-2-carboxylic acid (0.065 g, 0.33 mmol, 1.0 equiv) and HATU (0.250 g, 0.66 mmol, 2.0 equiv) at RT. The resulting reaction mixture was stirred for 10 minutes DIPEA (0.28 mL, 0.99 mmol, 3.0 equiv) was added. The reaction mixture was allowed to stir at RT overnight. Product formation was confirmed by LCMS. The reaction mixture was diluted with water (25 mL) and extracted with ethyl acetate (50 mL x 2). Combined organic layer was washed with water (20 mL x 4), dried over anhydrous NaaSOr and concentrated. The crude product was purified by reverse phase HPLC to obtain 5-chloro-N-(4-(2-(4-chloro-3-fluorophenoxy)acetamido)piperidin-l- yl)benzofuran-2-carboxamide (Compound 2 – 20 mg, 12 % yield) as an off white solid. LCMS 480 i H | +; H NMR (400MHz, DMSG-de) d 9 79 (s, 1 H), 8.08 (d, J= 7.5 Hz, 1 H), 7.86 (s, 1 H), 7.70 (d, J= 9.2 Hz, 1 H), 7.54 – 7.38 (m, 3 H), 7.08 (d, J= 8 8 Hz, 1 H), 6.86 (d, .7= 11.8 Hz, 1 H), 4.53 (s, 2 H), 3.66 (br. s., I H), 2.99 (br. s., 2 H), 2.78 (br. s, 2 H), 1.75 (br. s., 2 H), 1.66 (br. s., 2 H)

10242-10-1, 10242-10-1 5-Chlorobenzofuran-2-carboxylic acid 937838, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Patent; PRAXIS BIOTECH LLC; DELGADO OYARZO, Luz Marina; URETA DIAZ, Gonzalo Andres; PUJALA, Brahmam; PANPATIL, Dayanand; BERNALES, Sebastian; CHAKRAVARTY, Sarvajit; (0 pag.)WO2019/236710; (2019); A1;,
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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, A mixture of 3 -fluorophthalic anhydride (1 equiv.), 9-amino-S -(4-methoxybenzyl)-2-oxa- 6-thia-5-azaspiro[3.5]nonane 6,6-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 (Na2 SO4) and concentrated to provide 4-fluoro-2? -oxetano-6? -sulfonyl-thalidomide.

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

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

19477-73-7, 6-Bromoisobenzofuran-1(3H)-one is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

6-Bromophthalide was prepared by portion wise addition of phthalide (1 g, 7.45 mmol) to a mixture of trifluoroacetic acid (TFA) (3.7 mL) and sulfuric acid (1.7 mL) at room temperature for 9 h. The reaction mixturewas stirred at room temperature for 60 h, then poured onto ice and extracted with ethyl acetate. The combined organic phases were subsequently washed with a saturated solution of sodium bicarbonate and brine. After evaporation of the solvents in vacuum, the crude product was purified by column chromatography on silica gel (n-hexane/EtOAc: 9/1) to yield the desired product, 19477-73-7

19477-73-7 6-Bromoisobenzofuran-1(3H)-one 262235, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Article; Mirabdolbaghi, Roya; Dudding, Travis; Tetrahedron; vol. 69; 15; (2013); p. 3287 – 3292;,
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37418-88-5, 4-Hydroxyisobenzofuran-1,3-dione is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 100 Preparation of 2-[4-[2-(6,7-bis(methoxymethyl)benzoxazol-2-ylthio]ethyl]piperazin-1-yl]-N-(2,6-di isopropylphenyl)acetamide: N,N-Diisopropylethylamine (4.39 g, 34.0 mmol) was added to a solution of 3-hydroxyphthalic anhydride (5.0 g, 30.5 mmol) in dichloroethane (60 ml), then chloromethyl methyl ether (2.57 g, 32.0 mmol) was dropped thereinto under cooling with ice water and the mixture was returned to room temperature and stirred for 1 hour. Then N,N-diisopropylethylamine (2.20 g, 17.0 mmol) and chloromethyl methyl ether (1.28 g, 16.0 mmol) were further added thereto followed by stirring for 1 hour. After the reaction, the solvent was evaporated and the residue was diluted with water followed by extracting with ether. The organic layer was washed with water and a saturated sodium chloride solution successively and dried over anhydrous magnesium sulfate and the solvent was evaporated therefrom to provide 6.3 g (yield 99%) of 3-methoxymethyloxyphthalic anhydride as colorless oil., 37418-88-5

As the paragraph descriping shows that 37418-88-5 is playing an increasingly important role.

Reference£º
Patent; Kowa Company, Ltd.; US2004/38987; (2004); 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.209256-42-8,2,3-Dihydrobenzofuran-4-carbaldehyde,as a common compound, the synthetic route is as follows.

D. trans-3-(2,3-Dihydro-4-benzofuranyl)-2-pronenoic acid A solution of 2,3-dihydrobenzofuran-4-carboxaldehyde (8.42 g, 56.9 mmol) and malonic acid (11.86 g, 114 mmol) in pyridine (30 mL) and pyrrolidine (1 mL) was heated at reflux for 6 hr. The solution was cooled and poured into cold water (400 mL). The mixture was made strongly acidic with 12 N HCl to give a pale yellow precipitate that was filtered and air dried. The pale yellow powder was recrystallized from isopropanol to give white flakes (10.3 g, 95.3%, mp: 205-207C). Anal. for C11H10O3: Calc’d, C, 69.46; H, 5.30. Found, C, 69.36; H, 5.17. 1H NMR (300 MHz, CDCl3) delta7.76 (d, 1H, J=16.1 Hz), 7.15 (t, 1H, J=7. 8 Hz), 7.07 (d, 1H, J=7.8 Hz), 6.81 (d, 1H, J=7.8 Hz), 6.37 (d, 1H, J=16.1 Hz), 4.62 (t, 2H, J=8.8 Hz), 3.33 (t, 2H, J=8.8 Hz)., 209256-42-8

209256-42-8 2,3-Dihydrobenzofuran-4-carbaldehyde 18787449, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; EP1041980; (2005); B1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem