Category: benzofuran

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.496-41-3,Benzofuran-2-carboxylic acid,as a common compound, the synthetic route is as follows.

324.0 mg (2 mmol) of benzofuran-2-carboxylic acid was suspended in 5 mLs of methylene chloride. The flask was flushed with argon for 10 minutes before injection of 0.4 mL (4 mmol) oxalyl chloride. Two drops of dimethylformamide were injected and furious bubbling began. The sealed vessel was continuously flushed with argon and vented for 2 hours at room temperature. 10 mLs of sieve dried ethanol was slowly injected and allowed to stir for an additional hour. Volatiles were removed under vacuum and the crude intermediate was resuspended in 5 mLs ethanol. To this solution was added 250 mg (5 mmol) of hydrazine water salt. The reaction was refluxed for 3 hours to give the corresponding hydrazide. Volatiles were removed under vacuum and the product suspended in 10 mLs of ethanol. From here the reaction proceeded as described in Series 1 General Procedure to yield 369.1 mg of dry product (72% yield). ?H NMR (400 MHz, DMSO): 10.26 (d, J 6.0 Hz, 1H),7.78 (d, J 8.0 Hz, 1H), 7.66 (d, J 8.4 Hz, 1H), 7.54 (s, 1H), 7.49-7.45 (m, 1H), 7.36-7.32 (m, 1H), 5.16-5.13 (m, 1H), 2.84-2.79 (m, 2H), 1.48-1.41 (m, 2H), 1.39-1.33 (m, 2H), 0.90 (t, J= 7.2 Hz,3H); ?3CNMR(100MHz,DMSO): 157.7, 154.7, 148.7, 127.5, 127.2, 124.2, 123.1, 112.2, 109.6, 51.2, 30.2, 20.3, 14.4. [(m+H)/z = 233.25]. (2254) purity 98.8%, tR 11.53 mins.

496-41-3, The synthetic route of 496-41-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MUSC FOUNDATION FOR RESEARCH DEVELOPMENT; CHOU, Chung-Jen, James; MCCLURE, Jesse; ZHANG, Cheng; INKS, Elizabeth; (68 pag.)WO2018/71740; (2018); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

64169-34-2, 5-Bromoisobenzofuran-1(3H)-one is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

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, 1.72 mmol), palladium (II) acetate (250 mg, 1.1 mmol) and 5-bromo-2-benzofuran-l(3H)-one (100 g, 470 mmol). DMF (1.88 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 (1.03 L, 516 mmol) was added via canula and the mixture was again degassed three times. The mixture was then heated at 85 C for 10 h. The mixture was then allowed to return to room temperature for overnight. 2-methylTHF (2L) 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-methylTHF. The organic layers were combined, washed three times with brine (4L each), dried over MgS04, filtered, and concentrated. The crude product 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., 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.; DONG, Shuzhi; PASTERNAK, Alexander; GU, Xin; FU, Qinghong; JIANG, Jinlong; DING, Fa-Xiang; TANG, Haifeng; DEJESUS, Reynalda, K.; SUZUKI, Takao; WO2015/100147; (2015); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

50551-63-8, 6-Methoxybenzofuran is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: To a reaction tube were added 20 mol % CuI, 20 mol % KI (or Xphos), 0.25 mmol heterocycles, 3.0 equiv DTBP, and 1.5 mL cyclic ethers under a nitrogen atmosphere. The resulting mixture was heated at 120 C. After 24 h, the solvent was removed under vacuum, and the residue was purified by flash chromatography (SiO2, petroleum ether/ethyl acetate10:1)., 50551-63-8

50551-63-8 6-Methoxybenzofuran 5314410, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Article; Wang, Chenyang; Gong, Ming; Huang, Mengmeng; Li, Yabo; Kim, Jung Keun; Wu, Yangjie; Tetrahedron; vol. 72; 49; (2016); p. 7931 – 7936;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13391-28-1,5-Methoxybenzofuran,as a common compound, the synthetic route is as follows.

prepared from 5-methoxybenzo[b]furan according to a similar demethylation method as described in WO 04/043904).

13391-28-1, As the paragraph descriping shows that 13391-28-1 is playing an increasingly important role.

Reference£º
Patent; N.V. Organon; US2007/112019; (2007); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

87-41-2, Isobenzofuran-1(3H)-one is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step (1) Preparation of 3-Bromophthalide A mixture of phthalide (7.5 g, 56 mmol) and N-bromosuccinimide (10 g, 55.5 mmol) in CCl4 (150 mL) was heated at reflux for 3 hours (reaction checked by TLC). The mixture was filtered hot and the filtrate was evaporated to dryness to yield the crude title compound (11.15 g, 97%). It was used as such in the next step.

87-41-2, As the paragraph descriping shows that 87-41-2 is playing an increasingly important role.

Reference£º
Patent; American Home Products Corporation; US4960902; (1990); A;,
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Benzofuran | C8H6O – PubChem

166599-84-4, Benzofuran-4-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(RS)-2-Cyclopropyl-2-[methyl-(2-methyl-5-phenyl-thiazole-4-carbonyl)-amino]-ethyl- ammonium chloride (0.17 mmol, 1.0 eq.) was suspended in DMF (0.2 ml) and a solution of benzofuran-4-carboxylic acid (0.135 mmol, 0.79 eq.) and DIPEA (0.57 mmol, 3.4 eq.) in DMF (0.54 ml) was added. Finally a solution of HATU (0.135 ml, 0.79 eq.) was added and the mixture was shaken overnight. The solvent was stripped off and the residue was purified by preparative HPLC yielding the desired product (0.0134 g, 22%)LC-MS: tR = 0.99; [M+H]+ = 460.18, 166599-84-4

166599-84-4 Benzofuran-4-carboxylic acid 22324117, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Patent; ACTELION PHARMACEUTICALS LTD; WO2009/22311; (2009); A2;,
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

35700-40-4, 2,3-Dihydrobenzofuran-7-carboxylic acid is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

c. Preparation of 5-nitro-2,3-dihydrobenzo[b]furan-7-carboxylic acid (15k) Method A: To an ice-cooled solution of 2,3-dihydrobenzo[b]furan-7-carboxylic acid (15a) (0.33 g, 2.0 mmol) in 3 ml of TFA there was added dropwise 0.6 ml of HNO3. At the end of 1 hour, the cooling bath was removed. After an additional 3 hours of stirring, the mixture was poured into ice-water. The precipitate was collected on a filter to give 0.22 g (52.6%) of crude 15k. This was recrystallized from ethyl acetate to provide 88 mg of acid 15k (21.4%), mp 249-251.5 C.

35700-40-4, 35700-40-4 2,3-Dihydrobenzofuran-7-carboxylic acid 2795014, abenzofuran compound, is more and more widely used in various fields.

Reference£º
Patent; Erbamont, Inc.; US4888353; (1989); A;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

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

Step 3. 2-(2, 3~dihydro-l-benzofuran-5-ylmethyl)-N,N-diethyl-l-(piperidin-4-ylmethyl)-lH- benzimidazole-5-carboxamide [0201] To a mixture of tert-butyl 4-[({2-amino-4-[(diethylamino)carbonyl]phenyl}amino)methyl]piperidine-l -carboxylate (Step 2 of Example 18, 0.047g, 0.12 mmol, 1 equiv), 2,3-dihydro-l-benzofuran-5-ylacetic acid (0.023g, 0.13 mmol, 1.1 equiv) and DMF (5 mL) were added DIPEA (24 muL, 0.14 mmol, 1.2 equiv) and HATU (0.049 g, 0.13 mmol, 1.1 equiv). The mixture was stirred at room temperature for 3 hours. Complete consumption of the starting material was confirmed by LC-MS. DMF was removed under reduced pressure. Dichloromethane was added to the resulting residue. The organic layer was washed once with a saturated aqueous NaHCOs solution, once with brine and dried over anhydrous Na2SO4. Dichloromethane was removed under reduce pressure. The resulting residue was dissolved in dichloroethane (3 mL) and a few drops of concentrated HCl were added. The mixture was stirred at 80 C for 2 hours. Complete consumption of the starting material was confirmed by LC-MS. Dichloromethane was added. The organic layer was washed once with a 2M aqueous NaOH solution, once with brine and dried over anhydrous Na2SO4. Dichloromethane was removed under reduced pressure. The resulting residue was purified by reversed-phase HPLC (2 times) and lyophilized to afford 2-(2,3-dihydro-l-benzofuran-5- ylmemyl)-N,N-diemyl-l-(piperidin-4-ymiemyl)-lH-benzimidazole-5-carboxamide (0.007 mg) in 9% yield. 1H NMR (400 MHz, METHANOL-D4) delta ppm 1.08 – 1.18 (m, 3 H) 1.20 – 1.31 (m, 3 H) 1.45 – 1.59 (m, 2 H) 1.74 – 1.83 (m, 2 H) 2.02 -2.16 (m, 1 H) 2.74 – 2.85 (m, 2 H) 3.17 (t, J=8.69 Hz, 2 H) 3.33 – 3.40 (m, 2 H) 3.51 – 3.63 (m, 2 H) 4.28 (d, .7=7.42 Hz, 2 H) 4.42 (s, 2 H) 4.53 (t, J=8.79 Hz, 2 H) 6.74 (d, J-8.20 Hz, 1 H) 7.03 – 7.08 (m, 1 H) 7.15 – 7.19 (m, 1 H) 7.44 (dd, /=8.40, 1.17 Hz, 1 H) 7.68 (s, 1 H) 7.77 (d, J=8.59 Hz, 1 H); MS (ESI) m/z 447.0 (M+H)+; Anal. Calcd (%) for C27H34N4O2 + 2.1 TFA + 1.5 H2O: C, 52.55; H, 5.53; N, 7.86. Found: C, 52.48; H, 5.48; N 7.96.

As the paragraph descriping shows that 69999-16-2 is playing an increasingly important role.

Reference£º
Patent; ASTRAZENECA AB; WO2007/91950; (2007); A1;,
Benzofuran – Wikipedia
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

Preparation of 1-(2,3-dihydrobenzofuran-5-yl)ethanone Into a 500 mL 3-necked round-bottom flask, was placed a solution of acetyl chloride (62 g) in dry dichloromethane (400 mL). To this was added aluminum(III) chloride (55.6 g, 1.00 equiv). The mixture was allowed to react, with stirring, for 30 min at -10 C. (solution A). Into another 2000 nm 3-necked round-bottom flask, was placed a solution of 2,3-dihydrobenzofuran (50 g, 0.42 mmol, 1.00 equiv) in dry dichloromethane (500 mL) at -10 C. The solution A was added to the above via a cannula, and was stirred for 30 min at 0 C. The mixture was poured into ice/HCl (5:1 v/v, 1 L). The resulting solution was allowed to react, with stirring, for an additional 2 h while the temperature was maintained at room temperature. The resulting solution was extracted three times with 500 mL of CH2Cl2 and dried over Na2SO4 and concentrated by evaporation under vacuum using a rotary evaporator. The residue was purified by eluding through a column with a 1:100 EtOAc/PE solvent system. This resulted in 67 g (94%) of 1-(2,3-dihydrobenzofuran-5-yl)ethanone as a yellow solid., 496-16-2

The synthetic route of 496-16-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MEMORY PHARMACEUTICALS CORPORATION; US2008/318941; (2008); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem