Heterocyclic Building Block-benzofuran

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.57319-65-0,6-Aminoisobenzofuran-1(3H)-one,as a common compound, the synthetic route is as follows.,57319-65-0

Example 68; 2-(3-Oxo-l,3-dihydro-isobenzofuran-5-yIcarbamoyl)-pyrrolidine-l-carboxylic acid benzyl ester (Compound 6068)Using General Procedure C from 0.075 g (0.5 mmol) of 6-Amino-3H- isobenzofuran- 1 -one. MS : 381.1 (M+H4). General Procedure C; A mixture of (S)-Pyrrolidine-l,2-dicarboxylic acid 1-benzyl ester (F.W. = 249.27, 0.15 g, 0.6 mmol), HATU (F.W. = 380.25, 0.209 g, 0.55 mmol), and DIEA (0.1 mL, 0.76 mmol) in DMF (5 mL) was stirred at room temperature for 1 h.. This mixture had to be prepared each time for the reactions of the amines described in the following Examples. The individual mixtures were stirred at room temperature for 20 h., then filtered and separated by reverse phase HPLC (20-100% of buffer B; buffer A: water containing 0.1% TFA; buffer B: MeCN containing 0.1%TFA). The combined fraction was evaporated to dryness to furnish the desired products.

The synthetic route of 57319-65-0 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GENELABS TECHNOLOGIES, INC.; WO2007/70556; (2007); A2;,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.58546-89-7,Benzofuran-5-amine,as a common compound, the synthetic route is as follows.,58546-89-7

To a suspension of 7-chloro-3-(4-fluorophenyl)pyrazolo[ 1 ,5-a]pyrimidine (350 mg, 1.42 mmol) in anhydrous acetonitrile (10 mL), was added DIPEA (740 muL, 4.25 mmol) and benzofuran-5 -amine (270 mg, 2.03 mmol). The mixture was stirred at 170 0C for 3 x 15 minutes, under microwave activation, then cooled to room temperature. Upon cooling a crystalline solid precipitated, this solid was filtered, washed with acetonitrile and dried in vacuo, giving 320 mg (66 %) of the title compound. LC-MS RT= 2.36 min, MH+ = 345.2. 1H NMR (de-DMSO): 10.15 (IH, s), 8.78 (IH, s), 8.30-8.23 (3H, m), 8.10 (IH, d, J2.2), 7.77 (IH, d, J2.2), 7.73 (IH, d, J 8.6), 7.43 (IH, dd, J 8.6 &; 2.2), 7.28 (2H, t, J 9.0), 7.04 (IH, d, J2.3), 6.25 (IH, d, J5.2).

The synthetic route of 58546-89-7 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BioMarin IGA, Ltd.; WREN, Stephen Paul; WYNNE, Graham Michael; LECCI, Cristina; WILSON, Francis Xavier; WO2010/86040; (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,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).

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

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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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

In a 50 ml flask was placed 3-Fluorophthalic anhydride (1.0 g, 6 mmol) and aqueous NH3 (1.6 g, 24 mmol). The mixture was heated to 280 0C within 30 minutes and then the flask was cooled to room temperature. 0.93 g of compound 13 were isolated as a yellow solid. LC-MS (ESI, positive): 166 [M+H]+.

The synthetic route of 652-39-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PHENOMIX CORPORATION; WO2008/86161; (2008); A1;,
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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,69999-16-2

(A) Preparation of 5-(2-hydroxyethyl)-2,3-dihydrobenzofuran STR76 A solution of (2,3-dihydrobenzofuran-5-yl)acetic acid (4.9 g — see EP-A-132130) in anhydrous tetrahydrofuran (50 ml) was added over 10 minutes, dropwise, to a stirred suspension of lithium aluminium hydride (1.57 g) in anhydrous tetrahydrofuran (50 ml) at 0. The mixture was allowed to warm to room temperature and stirred for 1 hour. Water (1.5 ml) was then added dropwise with caution followed by 10% aqueous sodium hydroxide (1.5 ml) and, finally, water (4.5 ml). The mixture was filtered and the inorganic salts washed with ethyl acetate (2*50 ml). The filtrate and washings were combined and concentrated in vacuo to give the title compound as an oil, yield 3.3 g. 1 H N.M.R. (CDCl3) delta=7.10 (s, 1H); 7.00 (d, 1H); 6.75 (m, 1H); 4.65-4.55 (m, 2H); 3.90-3.75 (m, 2H); 3.30-3.15 (m, 2H); 2.90-2.80 (m, 2H); 1.85-1.75 (brs, 1H) ppm.

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

Reference£º
Patent; Pfizer Inc.; US5192765; (1993); A;,
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66826-78-6, 5-Bromo-2,3-dihydrobenzofuran is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

PREPARATION 108 2,3-Dihydrobenzofuran-5-ylboronic Acid Obtained as a colourless solid (38%), m.p. >240 C.(decomp.), from 5-bromo-2,3-dihydrobenzofuran (Synthesis, 1988, 952) and trimethyl borate, using the procedure of Preparation 101. delta(DMSOd6): 3.33 (t,2H), 4.48 (t,2H), 6.68 (d,1H), 7.56 (d,1H), 7.63 (s,1H), 7.70 (brs,2H).

66826-78-6 5-Bromo-2,3-dihydrobenzofuran 2776159, abenzofuran compound, is more and more widely used in various.

Reference£º
Patent; Pfizer INC; US6387931; (2002); B1;,
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1914-60-9, 2,3-Dihydrobenzofuran-2-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To Intermediate 7 (0.05 g, 0.14 mmol) were added HATU (0.11 g, 0.28 mmol) and the appropriate carboxylic acid (0.18 mmol). The mixture was dissolved in DMF (5 mL) and DIPEA (0.11 mL, 0.64 mmol) was added. The mixture was stirred under nitrogen at r.t. for 72 h. The residue was concentrated in vacuo and purified by preparative HPLC, to yield the title compound as an off-white solid.

1914-60-9 2,3-Dihydrobenzofuran-2-carboxylic acid 2776555, abenzofuran compound, is more and more widely used in various.

Reference£º
Patent; UCB PHARMA S.A.; KATHOLIEKE UNIVERSITEIT LEUVEN, K.U.LEUVEN R&D; FORD, Daniel James; FRANKLIN, Richard Jeremy; GHAWALKAR, Anant Ramrao; HORSLEY, Helen Tracey; HUANG, Qiuya; REUBERSON, James Thomas; VANDERHOYDONCK, Bart; WO2014/96423; (2014); A1;,
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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.77095-51-3,Benzofuran-6-carboxylic acid,as a common compound, the synthetic route is as follows.

l-benzofuran-6-carboxylic acid (5.0 g) was charged in dichloromethane and added thionyl chloride (4.5 g) followed by stirring to get clear solution. The solvent was removed under reduced pressure, MDC (20 ml) was charged to the residue. The acid chloride, in methylene chloride was added slowly to a solution of (S)-2-(5,7-dichloro-l,2,3,4- tetrahydroisoquinoline-6-carboxamido)-3-(3-(methyl sulfonyl)phenyl)propanoic acid (13.8 g) and diisopropylethyl amine (10 ml) below 5C. Reaction mass was stirred at 0-5C till, completion of reaction. Reaction mass was then quenched with water 25ml. Layers were separated and organic layer washed with sodium bicarbonate solution. Organic layer concentrated to get crude Lifitegrast. Crude lifitegrast was recrystaliized in acetone. (13 g, yield-72.8%)

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

Reference£º
Patent; MANKIND PHARMA LTD.; BHAVSAR, Jigar Tarun Kumar; TIWARI, Rakesh; BHASHKAR, Bhuwan; KUMAR, Anil; (30 pag.)WO2019/73325; (2019); A1;,
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59434-19-4, 4-Aminophthalide is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a stirred mixture of 3-(diethoxymethyl)benzaldehyde (3.75 g, 18 mmol) and anhydrous sodium sulfate (21.3 g, 150 mmol) in anhydrous dichloromethane (300 mL) was added 4-aminoisobenzofuran-1(3H)-one (2.24 g, 15 mmol) at 0 C. After the addition, the mixture was stirred at room temperature for 6 days. The mixture was filtered and the cake was washed with dichloromethane (50 mL¡Á3). The filtrate was concentrated to give crude product. The crude product was washed with petroleum ether to give (E)-4-(3-(diethoxymethyl)benzylideneamino)isobenzofuran-1(3H)-one (3.1 g, yield 61%) as a white solid. LC-MS (ESI) m/z: 340 (M+1)+

59434-19-4 4-Aminophthalide 12284649, abenzofuran compound, is more and more widely used in various.

Reference£º
Patent; LEAD THERAPEUTICS, INC.; US2010/35883; (2010); A1;,
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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.66826-78-6,5-Bromo-2,3-dihydrobenzofuran,as a common compound, the synthetic route is as follows.

(i) Production of Ethyl 2,3-Dihydronaphtho[2,3-b]furan-6-carboxylate 5-Bromo-2,3-dihydrobenzofuran (38.86 g), which was prepared according to the literature (Alabaster, Ramon J. et al., Synthesis, 1988, vol. 12, pp950.), was dissolved in THF (300 mL) and cooled to -78 C. n-Butyl-lithium in hexane (1.6M; 160 mL) was added to the solution and stirred for 30 min. DMF (40 mL) was added to the mixture and was allowed to warm to room temperature. Water was added to the mixture and the solvent was evaporated. The residue was diluted with ethyl acetate, washed with water and brine, dried and concentrated to give crude product of 5-formyl-2,3-dihydrobenzofuran (28.47 g) as an oil.

As the paragraph descriping shows that 66826-78-6 is playing an increasingly important role.

Reference£º
Patent; Takeda Chemical Industries, Ltd.; US6649643; (2003); B1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem