Category: 77095-51-3

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.77095-51-3,Benzofuran-6-carboxylic acid,as a common compound, the synthetic route is as follows.,77095-51-3

e) Example 3.5 (10 mmol) was mixed with EDC (2.11 g, 11 mmol), ) N, N-dimethylaminopyridine (“DMAP”, 0.1 g), triethylamine (2.02 g) and Example 1.11 (1.62g, 10 mmol) in anhydrous DMF (50 mL). After 15 hours at room temperature, the reaction mixture was diluted with ethyl acetate (200 mL), washed with water (30 mL, 3 times), dried with anhydrous magnesium sulfate and filtered. The residue after concentration of the filtrate was purified by column eluting with 10-30% ethyl acetate in hexane to give the title compound (3.7 g, 92%) : ESI-MS (m/z) : (M+1) 213.1.

As the paragraph descriping shows that 77095-51-3 is playing an increasingly important role.

Reference£º
Patent; SUNESIS PHARMACEUTICALS, INC.; WO2005/44817; (2005); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

77095-51-3, Benzofuran-6-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,77095-51-3

100 mL of DCM were added to the Compound lll-HCI solution in DMSO as obtained in step A-example 2) and the mixture was cooled to 0 – 5 C. Benzofuran-6-carboxylic acid solution obtained in section A was added dropwise maintaining the temperature below 5 C. The mixture was stirred at 0 – 5 C for 2 h. (0194) After reaction completion 850 mL of water and 850 mL of DCM were added maintaining the temperature below 10 C. After phase separation the aqueous phase was extracted with 400 mL of DCM. Organic phases were mixed and washed three times with 400 mL of water. The organic phase was distilled to almost dryness, 470 mL of acetone were added and then the remaining DCM was distilled. The solution was filtered through a 0,2 muetaeta filter. 240 mL of water were added and then dicyclohexylamine was added until pH = 8.3. The mixture was stirred at 20 – 25 C for 16 h and then cooled to 0 – 10 C and stirred for additional 25 h. The product was filtered, then washed twice with 200 mL of water and dryed in the oven at 50 C. Yield: 65% HPLC purity: 99% Chiral HPLC purity > 99.5%

The synthetic route of 77095-51-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; INTERQUIM, S.A.; BERZOSA RODRIGUEZ, Xavier; MARQUILLAS OLONDRIZ, Francisco; (38 pag.)WO2019/20580; (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.77095-51-3,Benzofuran-6-carboxylic acid,as a common compound, the synthetic route is as follows.

77095-51-3, A. 2-(4-Bromobutyl)benzofuran-6-carboxylic acid n-Butyllithium solution (2.29 M in hexane, 44 ml., 0.1 mole) is added to a solution of diisopropylamine (10.1 g., 0.1 mole) in tetrahydrofuran (150 ml.) and hexamethylphosphoramide (15 ml.). The resulting solution is treated with benzofuran-6-carboxylic acid (8.1 g., 0.05 mole) and then with 1,4-dibromobutane (10.8 g., 0.05 mole) at 0 C. The mixture is stirred at 0 C. for 6 hours. It is then quenched with water, acidified with hydrochloric acid and extracted with ethyl acetate. Evaporation of the solvent gives 2-(4-bromobutyl)benzofuran-6-carboxylic acid.

77095-51-3 Benzofuran-6-carboxylic acid 17867234, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Patent; Merck & Co., Inc.; US4238487; (1980); A;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

77095-51-3, Benzofuran-6-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

77095-51-3, Add HATU (418 mg, 1.1 mmol) and DIPEA (390 mg, 3 mmol) to a vigorously stirred solution of benzofuran-6-carboxylic acid (178 mg, 1.1 mmol) in DMF (5 mL). After the reaction mixture was reacted at room temperature for 1 hour, (S)-2-(8-chloro-2,3-dihydro-1H-pyrrole[3,2,1-ij]-quinazoline-7-carbonylamino)- 3-(3-(Methanesulfonyl)phenyl)propanoic acid benzyl ester trifluoroacetate (649 mg, 1 mmol), the mixture was stirred at room temperature for 2 hours. Ethyl acetate was added (100 mL), sequentially washed with water (20mL), saturated brine (20mL) was washed, and the organic phase was dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated, the residue was purified by flash chromatography, Petroleum ether with 50% ethyl acetate in hexanes to afford the desired product as a white solid (661mg, 0.95mmol 95%).

The synthetic route of 77095-51-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Weimou Bio-technology (Shanghai) Co., Ltd.; Shen Wang; Ding Yue; Wang Jiangfeng; Jiang Hao; Chen Fuli; Wu Xinglong; Li Cunfei; Yang Liguo; Hu Biao; (34 pag.)CN109721605; (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.77095-51-3,Benzofuran-6-carboxylic acid,as a common compound, the synthetic route is as follows.

77095-51-3, 16.05 g (0.10 mol) of benzofuran-6-carboxylic acid (compound III) were added over a suspension of 16.05 g (0.10 mol) of 1 ,T-carbonyldiimidazole in 400 mL of ethyl acetate at 20-25 C, under nitrogen atmosphere. The mixture was stirred at 20-25 C for 1 hour, and the resulting solution was added over a mixture of 53.8 g (0.09 mol) of crude hydrochloride salt of benzyl (S)-2-(5,7-dichloro-1 ,2,3,4-tetrahydroisoquinoline-6- carboxamido)-3-[3-(methylsulfonyl)phenyl]propanoate (compound IV) as obtained in Example 1 and 37.6 ml. (0.22 mol) of /V,/V-diisopropylethylamine in a mixture of 200 ml. of ethyl acetate and 55 ml. of dimethylsulfoxide at 20-25 C. The resulting mixture was stirred at this temperature for 18 hours. 1.05 L of 0.5 M hydrochloric acid and 500 ml. of ethyl acetate were added. The organic phase was extracted, washed with 2 x 500 ml. of 4% (w/w) aqueous sodium bicarbonate and with 500 ml. of deionized water, in sequence. The organic layer was concentrated to dryness under reduced pressure, to give 63.1 g of benzyl (S)-2-[2-(benzofuran-6-carbonyl)-5,7-dichloro-1 ,2,3,4-tetrahydroisoquinoline-6- carboxamido]-3-[3-(methylsulfonyl)phenyl]propanoate (compound II) as a yellowish solid.

As the paragraph descriping shows that 77095-51-3 is playing an increasingly important role.

Reference£º
Patent; MEDICHEM, S.A.; BIN, Zhu; LINGXIANG, Rao; PUIG SERRANO, Jordi; DURAN LOPEZ, Ernesto; (28 pag.)WO2019/96996; (2019); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

77095-51-3, Benzofuran-6-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

77095-51-3, Benzofuran-6-carboxylic acid (compound of formula VI, 2.0 gm), N,N- Dimethylformamide (20 mL) and Triethylamine (3.74 gm) were charged into a 2000 mL RBF and the mixture was cooled to 10 C. HATU (5.63 gm) was charged into the mass and stirred for 30 minutes. Added above aqueous layer containing compound of formula II at 20 C and stirred for 1 hour. 1N aqueous hydrochloric acid (100 mL) was added and stirred for 10 minutes. Gummy solid was formed. The aqueous layer was decanted. Sodium carbonate solution (100 mL) and ethylacetate (60 mL) were added to the gummy mass and stirred for 30 minutes. Layers separated and the aqueous layer was washed with ethylacetate (60 mL). The aqueous layer was acidified with 1 N aqueous hydrochloric acid (100 mL) and stirred for 30 minutes. The precipitation was faltered and the wet solid was washed with water (20 mL). The solid was dried under vacuum at 50 C for 3 hours to yield 1 .5 gm of Lifitegrast. Purity: 94.85% by HPLC.

77095-51-3 Benzofuran-6-carboxylic acid 17867234, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Patent; DR. REDDY’S LABORATORIES LIMITED; ACHANTA, Srinivas; CHAKKA, Ramesh; DAHANUKAR, Vilas Hareshwar; CHANDRASEKHAR, Elati Ravi Rama; BHIMAVARAPU, Srinivasa Reddy; MADARABOINA, Mahendar; (35 pag.)WO2019/26014; (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.77095-51-3,Benzofuran-6-carboxylic acid,as a common compound, the synthetic route is as follows.,77095-51-3

[00142] The benzofuran carboxylic acid 18? was treated with oxalyl chloride (1.2 equivalents) and a catalytic amount of DMF, stirring for 5.5 hours until a clear solution was obtained. The solvent was removed under reduced pressure and the acid chloride of compound 18? was stored under argon until use, on the next day. The acid chloride, in methylene chloridewas added slowly to a methylene chloride solution of the compound of Formula 12 and diisopropylethylamine (DIPEA) which was cooled to 0-5 C. The reaction was not permitted to rise above 5C, and after completion of addition, was stirred at 5C for a further 0.5 hour. Upon aqueous workup and extraction with methylene chloride, the product, compound 19, was isolated in quantitative yield.

The synthetic route of 77095-51-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; SARCODE BIOSCIENCE INC.; ZELLER, James, Robert; VENKATRAMAN, Sripathy; BROT, Elisabeth, C.A.; IYER, Subashree; HALL, Michael; WO2014/18748; (2014); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

77095-51-3, Benzofuran-6-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

77095-51-3, Benzofuran-6-carboxylic acid (50.0 g, 0.308 moles), toluene and a catalytic amount of dimethyl formamide (DMF) are added, in sequence, to a reactor in N2 atmosphere. The suspension is heated under stirring to 55¡À5C. SOCl2 (0.370 moles) dissolved in toluene is added slowly, maintaining the temperature at 55¡À5C until conversion is complete. The solution is then concentrated under vacuum until an almost solid yellow residue is obtained. Residue = 55.6 g, molar yield = quantitative. ?HNMR (300MHz, CDC13): d 8.32 (s,lH), 8.01 (dd,l H,J;=8.3 l Hz J2=l .34Hz), 7.87 (d, 1 H, =2.08 Hz), 7.69 (d, 1 H, J=8.31 Hz), 6.88 (br d, 1 H).

As the paragraph descriping shows that 77095-51-3 is playing an increasingly important role.

Reference£º
Patent; OLON S.P.A.; BERTOLINI, Giorgio; FELICIANI, Lazzaro; LONGONI, Davide; SADA, Mara; VALLI, Matteo; (22 pag.)WO2019/239364; (2019); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

77095-51-3, Benzofuran-6-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

77095-51-3, Oxalyl chloride (29.35 gm) was slowly added to a pre-cooled mixture of compound of formula-2 (25 gm), dimethylformamide (5 ml) and tetrahydrofuran (325 ml) at 0-5C under nitrogen atmosphere. Raised the temperature of the reaction mixture to 25-30C and stirred for 5 hr at the same temperature. A solution of pentafluorophenol (31.21 gm) in tetrahydrofuran (25 ml) was added to the reaction mixture at 25-30C. Cooled the reaction mixture to 0-5C and Nu,Nu-diisopropylethyl amine (99.64 gm) was slowly added to it at the same temperature. Raised the temperature of the reaction mixture to 25-30C and stirred for 90 min at the same temperature. Methyl tert.butyl ether and water were added to the reaction mixture at 25-30C and stirred the reaction mixture for 10 min at the same temperature. Both the organic and aqueous layers were separated and washed the organic layer with 10% aqueous sodium bicarbonate solution followed by with water. Distilled off the solvent completely from the organic layer and co-distilled with acetonitrile. Compound of formula- 4a (47.92 gm), acetonitrile (250 ml) and N,N-diisopropylethylamine (59.78 gm) were added to the obtained compound at 25-30C and stirred the reaction mixture for 40 min at the same temperature. Heated the reaction mixture to 60-65 C and stirred for 3 hr at the same temperature. Cooled the reaction mixture to 5-10C, 50% aq.HCl solution was slowly added to it and stirred the reaction mixture for 2 hr at the same temperature. Filtered the solid and washed with water. Ethyl acetate (175 ml) and water (250 ml) were added to the obtained compound at 25-30C. Slowly basified the reaction mixture by using 10% aqueous potassium carbonate solution (25 gm of potassium carbonate in 250 ml of water) at 25-30C and stirred the reaction mixture for 10 min at the same temperature. Both the organic and aqueous layers were separated and washed the aqueous layer with ethyl acetate. Slowly acidified the aqueous layer by using 50% aqueous hydrochloric acid solution (25 ml of hydrochloric acid in 25 ml of water) at 25-30C and stirred the reaction mixture for 3 hr at the same temperature. Filtered the solid, washed with acetone and dried the material to get the title compound. The PXRD pattern of the obtained compound is illustrated in figure- 1.

As the paragraph descriping shows that 77095-51-3 is playing an increasingly important role.

Reference£º
Patent; MSN LABORATORIES PRIVATE LIMITED, R&D CENTER; SRINIVASAN, Thirumalai Rajan; SAJJA, Eswaraiah; GHOJALA, Venkat Reddy; SAGYAM, Rajeshwar Reddy; RANGINENI, Srinivasulu; KOMMERA, Rajashekar; (71 pag.)WO2019/43724; (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.77095-51-3,Benzofuran-6-carboxylic acid,as a common compound, the synthetic route is as follows.,77095-51-3

Benzofuran carboxylic acid (II) (1.0 g, 6.17 mmol, 1.0 equiv), DMF (0.01 eq) and THF (10 mL, 10 vol) is charged to a two-neck round bottom flask under nitrogen atmosphere. Oxalyl chloride (1.1 mL, 13.34 mmol, 2.0 equiv) is slowly added while keeping the temperature between 20 to 30 C. The resulting solution was stirred at 20-30 C. for over 2 hr. When the reaction was complete as determined by TLC analysis, the solvent was removed under reduced pressure and the acid chloride of compound of Formula II (Formula IIb) was stored under nitrogen.

As the paragraph descriping shows that 77095-51-3 is playing an increasingly important role.

Reference£º
Patent; ScinoPharm Taiwan, Ltd.; WU, Ming-Chih; HSIAO, Tsung-Yu; US2019/2445; (2019); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem