Day: October 19, 2020

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

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

69999-16-2, 2,3-Dihydrobenzofuranyl-5-acetic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(S)-4-Bromo-3-hydrazono-2-oxo-2,3-dihydro- lH-indole-6-carboxylic acid [3-(2- hydroxymethyl-pyrrolidin-l-yl)-propyl]-amide (0.22 g, 0.52 mmol) was added to a solution of (2,3-dihydro-benzofuran-5-yl)-acetic acid (0.93 g, 0.52 mmol), triethylamine (0.01 mL, 0.78 mmol) and HBTU (0.20 g, 0.52 mmol) in DMF (4 mL) and stirred at room temperature overnight. The reaction mixture was concentrated in vacuo and purified by column chromatography (20% methanol in dichloromethane) followed by HPLC (10-100% acetonitrile/water) to give 0.040 g (13%) of (S)-4- bromo-3 – [(2-2,3 -dihy dro-benzof uran-5 -yl-acetyl)-hydrazono] -2-oxo-2,3 -dihydro- 1 H- indole-6-carboxylic acid [3-(2-hydroxymethyl-pyrrolidin-l-yl)-propyl]-amide. 1H NMR (400 MHz, CD3OD) 5 7.75 (s, IH), 7.37 (s, IH), 7.24 (s, IH), 7.11 (d, J = 7.8 Hz, IH), 6.65 (d, / = 8.2 Hz, IH), 4.50 (t, J = 12.7 Hz, 2H), 4.10 (bs, 2H), 3.88 (dd, J = 3.9 Hz, 7= 12.2 Hz, IH), 3.74-3.40 (m, 6H), 3.22-3.04 (m, 4H), 2.26-1.81 (m, 6H). Mass spectrum (LCMS, ESI pos.): Calcd for C27H30BrN5O5: 584.46; found 584.1(M+H). EPO

69999-16-2, The synthetic route of 69999-16-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; JANSSEN PHARMACEUTICA N.V.; WO2006/101937; (2006); 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.128851-73-0,6-Bromobenzofuran,as a common compound, the synthetic route is as follows.

1) In a dry 500mL three-necked flask, add 3-bromoaniline (17.20g, 100mmol) and 6-bromobenzofuran (19.70g, 100mmol), toluene (200mL) and sodium tert-butoxide (28.83g, 300mmol), ultrasonically remove the air, under the protection of nitrogen, add palladium acetate (0.07 g, 0.3 mmol) and tri-t-butylphosphine (0.18 g, 0.6 mmol) the reaction was heated under reflux at 115 C for 6 hours. The reaction was monitored by liquid phase. After cooling to room temperature, 1-bromonaphthalene (20.71g, 100mmol) was added, and the temperature was raised to 115 C to continue the reaction for 8h. The reaction was monitored in liquid phase to complete the reaction, cooled to room temperature, washed twice with water, and separated. The organic phase was dried over anhydrous magnesium sulfate, filtered, The filtrate was decolorized by adding activated carbon at 115 C for 30 minutes, hot filtration, and the filtrate was concentrated. After beating with ethanol twice, 30.07g of intermediate a can be obtained with a yield of 75%., 128851-73-0

The synthetic route of 128851-73-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Wuhan Shang Sai Optoelectric Technology Co., Ltd.; Mu Guangyuan; Zhuang Shaoqing; Ren Chunting; (42 pag.)CN110590568; (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.23145-07-5,5-Bromobenzofuran,as a common compound, the synthetic route is as follows.

23145-07-5, A. Preparation of 5-Cyanobenzo(b)furan: 5-Bromobenzo(b)-furan (19.3 g., 0.098 mole) was added dropwise to a stirred mixture of cuprous cyanide (0.14 mole) and pyridine at 165¡ã C. Heating at 165¡ã C. was continued for 26 hours and the cool reaction mixture was then added to 10percent (by weight) aqueous ammonia solution. Toluene (100 ml.) was added and the resulting mixture stirred for 0.5 hours and then filtered. Ether (250 ml.) was added to the filtrate and the organic phase separated and combined with the ether extracts (2*100 ml.) of the aqueous phase. The combined organic solutions were washed in turn with 5percent aqueous ammonia (4*100 ml.), water (100 ml.), dilute hydrochloric acid (3*100 ml.) and finally water (100 ml.). Evaporation in vacuo of the dried (MgSO4) organic solution gave an oil which readily solidified. Purification was effected by column chromatography on silica gel using methylene chloride as eluent. Trituration of the product with hexane provided pure 5-cyanobenzo(b)furan as a white solid (8.2 g), m.p. 85¡ã-87¡ã C. Analysis percent: Found: C, 75.2; H, 3.5; N, 9.7; C9 H5 NO requires: C, 75.5; H, 3.5; N, 9.8.

As the paragraph descriping shows that 23145-07-5 is playing an increasingly important role.

Reference£º
Patent; Pfizer Inc.; US4341792; (1982); 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.69999-16-2,2,3-Dihydrobenzofuranyl-5-acetic acid,as a common compound, the synthetic route is as follows.,69999-16-2

208 g of tetrahydrofuran was added to the reaction flask.Then add 13g (0.344mol) sodium borohydride,Add with stirring26g (0.146mol)Compound 1 obtained in Example 3,Insulation does not exceed 10C during the joining process.After the addition,49 g (0.345 mol) of boron trifluoride diethyl ether complex were initially added dropwise for about 2 hours.After dropping,The temperature of the dropping process does not exceed 15C.After the addition,Remove ice salt water,Naturally warm to room temperature;Reheat to reflux,After about 2hrs,After the reaction is completed,Cool down to 15C,Methanol 60 g was added dropwise.Then add 140g concentrated hydrochloric acid solution,After stirring,Tetrahydrofuran is concentrated under reduced pressureAfter the basic concentration of tetrahydrofuran is complete,An aqueous solution containing 11 g of sodium hydroxide is added,Add 300g ethyl acetate extraction,Liquid separation,The aqueous phase is extracted with 200 g of ethyl acetate.Combine the organic phase,Dry with anhydrous sodium sulfatefilter,Concentrate under reduced pressure,Get an oil,19.2g (theoretical quantity:23.96g);Yield:80.1%.

The synthetic route of 69999-16-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Inner Mongolia Jingdong Pharmaceutical Co., Ltd.; Guo Rongyao; Wang Xiaofeng; (9 pag.)CN107721954; (2018); A;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

24673-56-1, 3-Methylbenzofuran-2-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

3-Methylbenzofuran-2-carboxylic acid (commercially available) was heated withcopper metal in quinoline to give compound 5. Colorlessoil, 1H-NMR (500 MHz, CDCl3) delta: 2.22 (3H, d, J=1.2 Hz),7.18-7.26 (2H,m), 7.38 (1H, dd, J=1.2, 8.0 Hz), 7.48 (1H, m),7.51 (1H, dd, J=1.2, 8.0 Hz). 13C-NMR (125 MHz, CDCl3)delta: 6.4, 110.6, 115.2, 119.0, 121.9, 123.8, 128.4, 141.4, 155.5.Its spectral data are in accordance with previously reported data.

24673-56-1, The synthetic route of 24673-56-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Yamaguchi, Yuki; Akimoto, Ichie; Motegi, Kyoko; Yoshimura, Teruki; Wada, Keiji; Nishizono, Naozumi; Oda, Kazuaki; Chemical and Pharmaceutical Bulletin; vol. 61; 10; (2013); p. 997 – 1001;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem