Heterocyclic Building Block-benzofuran

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.

To a stirred solution of 6-bromobenzo[b]furan (100 mg, 0.507 mmol) in 1 ,4-dioxane (15 mL), tert-butyl 6-fluoro-3-(4,4,5,5-tetramethyl-1 ,3,2-dioxaborolan-2-yl)-1 H-indole-1 – carboxylate (Intermediate 2, 180 mg, 0. 507 mmol), K2CO3 (210 mg, 1 .52 mmol) and Pd(dppf)CI2 (19 mg, 0.025 mmol) were added. The mixture was stirred at 80 C for 15 hrs. The solvent was removed and the residue was purified by prep-TLC (EtOAc/Petroleum Ether=1 /10) to afford 1 12.8 mg (63%) of the title compound. LC-MS for C2iH18FNO3+H+ [M+H]+ : calcd: 351 .1 ; found: 351 .8. 1 H NMR (400 MHz, CDCI3) delta [ppm]: 7.96 (d, J = 4.8 Hz, 1 H), 7.79-7.76 (m, 2H),7.71 -7.67 (m, 3H),7.50 (dd, J = 8.0 Hz,1 .6Hz, 1 H),7.06 (dd, J = 8.8, 2.4 Hz, 1 H), 6.82 (d, J = 1 .0 Hz, 1 H), 1 .70 (s, 9H).

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

Reference£º
Patent; ITEOS THERAPEUTICS; CAUWENBERGHS, Sandra; CROSIGNANI, Stefano; DRIESSENS, Gregory; DEROOSE, Frederik; (271 pag.)WO2015/140717; (2015); 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.942-06-3,4,5-Dichlorophthalic Anhydride,as a common compound, the synthetic route is as follows.

To a solution of 5,6-dichloroisobenzofuran-1,3-dione (2 g, 9.22 mmol) in xylene (10 ml), 2-aminoacetic acid (0.761 g, 10.14 mmol) was added, and the reaction was heated at 160¡ã C. for 40 hours. The precipitate that formed during the reaction was filtered, washed with water and hexanes and dried affording 2-(5,6-dichloro-1,3-dioxoisoindolin-2-yl)acetic acid (2.33 g, 8.50 mmol, 92percent yield).

942-06-3 4,5-Dichlorophthalic Anhydride 70334, abenzofuran compound, is more and more widely used in various.

Reference£º
Patent; Chiesi Farmaceutici S.p.A.; ARMANI, Elisabetta; Amari, Gabriele; Capaldi, Carmelida; Carzaniga, Laura; La Porta, Elena; Guala, Matilde; US2013/102576; (2013); A1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

16859-59-9, 3-Hydroxyisobenzofuran-1(3H)-one is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

General procedure: 2-Formylbenzoic acid (1a; 1.0 equiv) was heated at reflux in SOCl2 (5?10 equiv) for 4 h at 100 ¡ãC. The remaining SOCl2 was removed in vacu-um and the obtained solid was dissolved in CH2Cl2 (10 mL). The mix-ture was cooled to 0 ¡ãC and the desired primary amine (2.0 equiv)was slowly added. The solution was stirred for 24 h at r.t. then thereaction mixture was diluted with EtOAc (70 mL), washed with citricacid (0.5 M), sat. aq Na2CO3 solution, and brine. The organic layer wasdried over MgSO4 and the solvent was removed under reduced pres-sure. The obtained products were used without further purification.

As the paragraph descriping shows that 16859-59-9 is playing an increasingly important role.

Reference£º
Article; Niedek, Dominik; Schuler, Soeren M.M.; Eschmann, Christian; Wende, Raffael C.; Seitz, Alexander; Keul, Felix; Schreiner, Peter R.; Synthesis; vol. 49; 2; (2017); p. 371 – 382;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

128851-73-0, 6-Bromobenzofuran is a benzofuran compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example 11 (2RS,3RS)-3-benzofuran-6-yl-1-dimethylamino-2-methylpentan-3-ol Hydrochloride(10) 3.45 g (18 mmole) 6-bromobenzofurane (prepared according to EP 355 827) and 6 ml 1,2-dibromoethane, dissolved in 60 ml dry ether, were added drop-wise over 1.5 hours to 2.12 g (87 mmole) magnesium turnings in 30 ml dry ether; after the addition the mixture was heated under reflux for 30 minutes. Thereafter, 2.5 g (18 mmole) 1-dimethylamino-2-methylpentan-3-one dissolved in 7.5 ml ether was added drop-wise over 1.5 hours whilst cooling in an ice bath to maintain an internal temperature of 5-10 C. The reaction mixture was allowed to stand for 12 hours at room temperature, and was then cooled again to 5-10 C. and added to 35 ml of 20% aqueous ammonium chloride solution. After phase separation, the aqueous phase was extracted twice with 50 ml ether. The combined organic phases were dried over sodium sulphate. After removing the solvent by distillation the residue (3.9 g) was introduced on to a 5*16 cm column packed with silica gel. 0.95 g of base were obtained by elution with 7:1 diisopropyl ether/methanol, from which 0.82 g of hydrochloride (10) (15.5% theoretical) with a melting point of 162 C. were obtained with trimethylchlorosilane/water in ethyl acetate/2-butanone.

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

Reference£º
Patent; Gruenenthal GmbH; US6248737; (2001); B1;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.127264-14-6,5-(2-Bromoethyl)-2,3-dihydrobenzofuran,as a common compound, the synthetic route is as follows.

This Example illustrates a process for preparing a compound of formula (IV). This Example also illustrates the conversion of a compound of formula (IV) to the hydrobromide salt.[0048] Into a reaction vessel were charged 2,2-diphenyl-2-[(35)-pyrrolidin-3- yl]acetamide L-(+)-tartrate (90.00 g, 0.21 mol), methyltriethylammonium chloride (4.82 g, 0.03 mol) and 2-methyltetrahydrofuran (180 mL). The resulting suspension was heated to 60-70 ¡ãC. To the suspension was added a solution of potassium hydroxide (69.79 g, 1.05 mol) in water (180 mL), keeping the temperature between 60 and 70 0C. The mixture was heated to reflux and to this mixture was added dropwise a solution of 5-(2-bromoethyl)-2,3- dihydro-1-benzofuran (56.98 g, 0.25 mol) in 2-methyltetrahydrofuran (270 mL). The resulting mixture was heated at reflux for 16 h and cooled to room temperature. The phases were separated and the organic phase was washed twice with 180 mL of a 10percent aqueous solution of ammonium chloride. The remaining water was distilled azeotropically and hydrobromic acid 48percent (28.19 mL) was added dropwise at room temperature. The resulting suspension was cooled to 0-5 ¡ãC, stirred at this temperature for 2 h and filtered. An almost white solid was obtained (188.0 g, l.o.d. = 48.83percent, 90.67percent yield, HPLC purity (method B): 98.96percent). This solid can be optionally dried at 60 ¡ãC under vacuum. This solid can be optionally further purified as in Example 4.[0049] The results demonstrate a process for preparing (S)-2- { 1 -[2-(2,3- dihydrobenzofuran-5-yl)ethyl]-3-pyrrolidinyl}-2,2-diphenylacetamide hydrobromide of formula (IV) in high yield and purity.

As the paragraph descriping shows that 127264-14-6 is playing an increasingly important role.

Reference£º
Patent; MEDICHEM, S.A.; WO2008/29257; (2008); A2;,
Benzofuran – Wikipedia
Benzofuran | C8H6O – PubChem