Day: October 19, 2020

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.130-03-0,Benzo[b]thiophen-3(2H)-one,as a common compound, the synthetic route is as follows.

General procedure: To a stirred mixture of ketone 1a or 1b (3 mmol) and diarylpropargylic alcohols 2a-e (3 ml) in acetonitrile (3 ml) the corresponding catalyst (Table 1) was added and the reaction mixture was refluxed under argon for 1 h. After cooling, the solvent was distilled off in vacuo. The residue was purified by recrystallization from the corresponding solvent or by chromatography on silica gel using the light petroleum/ethyl acetate (8:1) system as an eluent., 130-03-0

As the paragraph descriping shows that 130-03-0 is playing an increasingly important role.

Reference£º
Article; Shirinian, Valerii Z.; Zavarzin, Igor V.; Leonova, Evgeniya S.; Markosyan, Ashot I.; Mendeleev Communications; vol. 25; 4; (2015); p. 262 – 263;,
Benzothiophene – Wikipedia
Benzothiophene | C8H6S – PubChem

6314-28-9, Benzo[b]thiophene-2-carboxylic acid is a benzothiophene compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

6314-28-9, To a solution of benzo[t]thiophene-2-carboxylic acid (274 mg, 1.54 mmol) and 4- (tert-butyl)thiazol-2-amine (200 mg, 1.28 mmol) in DMF (0.84 mL) was added HATU (585 mg, 1.54 mmol) followed by DIEA (791 uL, 4.90 mmol). The mixture was heated to 80 C for 3 h then cooled to ambient temperature, diluted with ethyl acetate (5 mL) and brine (5 mL), and extracted with ethyl acetate (1X5 mL). The organics were combined, washed with brine (2X5 mL), dried with sodium sulfate, filtered, and concentrated. Flash chromatography (0-60% hexanes/ethyl acetate) provided N-(4-tert-butyl-1 ,3-thiazol-2-yl)-1 -benzothiophene-2- carboxamide (397 mg, 98% yield) as an off-white solid. (A145) H NMR (400 MHz, DMSO-d6) delta 12.92 (s, 1 H), 8.63 (s, 1 H), 8.38 – 7.81 (m, 2H), 7.71 – 7.29 (m, 2H), 6.85 (s, 1 H), 3.33 (s, 3H), 1.31 (s, 9H). LCMS for C16H16N202S, found 317 [M+H]+.

As the paragraph descriping shows that 6314-28-9 is playing an increasingly important role.

Reference£º
Patent; KEZAR LIFE SCIENCES; THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; MCMINN, Dustin; JOHNSON, Henry; TAUNTON, John, William; CARRASCO, Yazmin, Paulina; SHARP, Phillip, Patrick; (156 pag.)WO2019/46668; (2019); A1;,
Benzothiophene – Wikipedia
Benzothiophene | C8H6S – PubChem

95-15-8, Thianaphthene is a benzothiophene compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,95-15-8

EXAMPLE 1 N-(1-trans-(2-(benzo[b]thien-2-yl)cyclopropyl)ethyl)-N-hydroxyurea STR18 To a solution of benzo[b]thiophene (11.49 g, 85.6 mmol) in 300 mls THF at -78 C., was added n-butyllithium (36.0 mls of a 2.5 M solution in hexanes, B9.9 mmol) dropwise and the mixture was stirred for 30 mins at -78 C. N,N,-Dimethylformamide (6.57 g, 89.9 mmol) was added and the reaction was allowed to stir for 30 min. The cooling bath was then withdrawn and the reaction was allowed to warm to room temperature. It was then diluted with saturated aqueous NH4 Cl (250 mL) and extracted with ethylacetate (3*250 mL). The organics were combined, dried with MgSO4 and concentrated. The resulting residue was taken up in 20 mL ethanol and saturated aqueous NaHSO3 (200 mL) was added. The resulting precipitate was collected and washed with ether. It was then dissolved in saturated aqueous Na2 CO3 (200 mL) and the resulting aqueous solution was extracted with ethylacetate (3*200 mL). The organics were combined, dried with MgSO4 and concentrated to afford 13.63 g (98%) of benzo[b]thien-2-ylcarboxaldehyde.

The synthetic route of 95-15-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Abbott Laboratories; US5037853; (1991); A;,
Benzothiophene – Wikipedia
Benzothiophene | C8H6S – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5381-20-4,Thianaphthene-3-carboxaldehyde,as a common compound, the synthetic route is as follows.

5381-20-4, General procedure: Amixture of the heterocyclic salt I1-I16 (2.5 mmol), aldehyde (7.5 mmol, 3 molar equiv, unlessotherwise stated) and piperidine (0.50 mL, 5 mmol, 2 molar equiv) in EtOH (25 mL) was heatedunder reflux for 2.5 h. After cooling to room temperature, the precipitated solid was collectedby filtration, washed with EtOH (2 ¡Á 5 mL) and Et2O (2 ¡Á 5 mL) and dried. The crude iodidesalt was either purified through a recrystallization from a suitable solvent (as indicated below)to give an analytically pure sample, or subjected to anion exchange to bromide or chloride, asdescribed below. Procedure for anion exchange: Ion-exchange resin (Amberlite IRA-402, Cl- form, or AmberliteIRA-400, Br- form, about 20 mmol equiv) was thoroughly rinsed with a mixture of MeCN andMeOH (1:1, v/v) and charged into a short glass column. The dye (iodide salt) was dissolvedin a minimal amount of a mixture of MeCN and MeOH (1:1, v/v) and loaded in the column. Theproduct was then eluted with the same solvent mixture (about 50 mL). The solvents wereremoved in vacuo and the residue was recrystallized from a suitable solvent (as indicatedbelow), to give an analytically pure dye.

The synthetic route of 5381-20-4 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Xie, Xiao; Zuffo, Michela; Teulade-Fichou, Marie-Paule; Granzhan, Anton; Beilstein Journal of Organic Chemistry; vol. 15; (2019); p. 1872 – 1889;,
Benzothiophene – Wikipedia
Benzothiophene | C8H6S – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.6314-28-9,Benzo[b]thiophene-2-carboxylic acid,as a common compound, the synthetic route is as follows.

6314-28-9, General procedure: The DCC (1.2 equiv) was added to the solution of caudatin(0.2 mmol), DMAP (0.2 equiv), and appropriate carboxylic acid (1.2 equiv) in anhydrous CH2Cl2 (8 mL) at 0 C.The resulting mixture was stirred at room temperature until the starting material was not observed by TLC. The reaction mixture was filtered, and the residue was washed with CH2Cl2 (210 mL). Then, the CH2Cl2 solution was washed with 5% HCl (330 mL), saturated NaHCO3 (330 mL) and saturated NaCl (330 mL), respectively. Subsequently, the organic layer was dried by Na2SO4 and concentrated to dryness under reduced pressure. At last, the residue was purified by column chromatography over the silica gel with petroleum ether/acetone (60:40 – 95:5) to yield the pure target compounds.

6314-28-9 Benzo[b]thiophene-2-carboxylic acid 95864, abenzothiophene compound, is more and more widely used in various fields.

Reference£º
Article; Wang, Li-Jun; Chen, Hao; Ma, Yun-Bao; Huang, Xiao-Yan; Geng, Chang-An; Zhang, Xue-Mei; Chen, Ji-Jun; Medicinal Chemistry; vol. 11; 2; (2015); p. 165 – 179;,
Benzothiophene – Wikipedia
Benzothiophene | C8H6S – PubChem

360576-01-8, Methyl 6-bromobenzo[b]thiophene-2-carboxylate is a benzothiophene compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of compound B-110 (2.7 g, 10 mmol) and cyclopropylboronic acid (0.73 g, 10 mmol) in anhydrous toluene (50 mL) under N2 was added tetrakis(triphenylphosphine)palladium(0) (0.54 g, 0.47 mmol), followed by a solution of potassium phosphate (3.2 g, 15 mmol) in water (5 mL). The solution was stirred at room temperature for 0.5 hour before being heated to reflux for 7 hours. On completion, the mixture was cooled to room temperature and filtered. The filtrate was concentrated and purified by silica gel chromatography [petroleum ether: ethyl acetate = 60: 1] to give compound B-lll (1.8 g, 70% yield) as a white solid. LCMS: (ES+) m/z (M+H)+ = 233.0., 360576-01-8

360576-01-8 Methyl 6-bromobenzo[b]thiophene-2-carboxylate 22474078, abenzothiophene compound, is more and more widely used in various fields.

Reference£º
Patent; FORUM PHARMACEUTICALS, INC.; ACHARYA, Raksha; BURNETT, Duane, A.; BURSAVICH, Matthew, Gregory; COOK, Andrew, Simon; HARRISON, Bryce, Alden; KOENIG, Gerhard; MCRINER, Andrew, J.; (400 pag.)WO2016/100184; (2016); A1;,
Benzothiophene – Wikipedia
Benzothiophene | C8H6S – PubChem

20699-85-8, Methyl 5-aminobenzo[b]thiophene-2-carboxylate is a benzothiophene compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 5-amino- benzo[b]thiophene-2-carboxylic acid methyl ester (989 mg, 4.79 mmol) in CH2CWTHF (5/5 mL) was added NMM (630 muL, 5.73 mmol) and chloroacetylchloride (415 muL, 5.25 mmol). After stirring 2.5 h, the mixture was diluted with EtOAc and H2O, and the solid was filtered yielding a pale-white solid, which was used without exp (MH+) 284.

20699-85-8, The synthetic route of 20699-85-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; MERCK & CO., INC.; ATON PHARMA, INC.; WO2006/115845; (2006); A1;,
Benzothiophene – Wikipedia
Benzothiophene | C8H6S – PubChem

95-15-8,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.95-15-8,Thianaphthene,as a common compound, the synthetic route is as follows.

To a 13¡Á100 mm borosilicate glass heavy wall test tube was added benzothiophene (73.8 mg, 0.55 mmol). A stock solution of Pd(OAc)2 (16.8 mg, 0.075 mmol, 75 mM) and BQ (8.1 mg, 0.075 mmol, 75 mM) in 1.0 mL DMSO was created. A stock solution of Cu(OAc)2.H2O (57.1 mg, 0.286 mmol, 143 mM) and phd (60.1 mg, 0.286 mmol, 143 mM) in 2.0 mL DMSO was created. Then, 100 muL DMSO, followed by 220 muL (0.0165 mmol) of the Pd(OAc)2/BQ stock solution, and 115 muL (0.0164 mmol) of the Cu(OAc)2.H2O/phd stock solution were added to the test tube. The test tube with reaction mixture was placed on an orbital mixing block with heating element. The mixing block was sealed, purged with O2 for five minutes, cooling water was turned on, and then the block was heated to 120 C. under 1 atm O2 with shaking for 48 hours. After 48 hours, the shaking was stopped, the block was depressurized, and the reaction test tube was removed and allowed to cool. An aliquot of a stock solution of 1,3,5-trimethoxybenzene in THF was added to the reaction mixture, and the DMSO/THF mixture was filtered through the Celite, and then the Celite was washed once more with THF. The filtrate was diluted with additional THF, and then it was shaken so that everything was evenly mixed.

As the paragraph descriping shows that 95-15-8 is playing an increasingly important role.

Reference£º
Patent; Wisconsin Alumni Research Foundation; Stahl, Shannon; Tereniak, Stephen; (42 pag.)US2019/210993; (2019); A1;,
Benzothiophene – Wikipedia
Benzothiophene | C8H6S – PubChem

346592-74-3, 7-Fluorobenzo[b]thiophene is a benzothiophene compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Step 1 3-[(7-Fluoro-benzo[b]thiophen-2-yl)-hydroxy-methyl]-3-(tetrahydro-pyran-4-ylmethyl)-pyrrolidine-1-carboxylic acid tert-butyl ester To a solution of 7-fluoro-benzothiophene (0.22 g, 1.44 mmoles) in anhydrous tetrahydrofuran (10 ml) at -78 C. was added dropwise a solution of n-BuLi in hexane (1.6M, 0.9 ml, 1.44 mmoles). The reaction mixture was stirred at -78 C. for one hour, and then a solution of 3-formyl-3-(tetrahydro-pyran-4-ylmethyl)-pyrrolidine-1-carboxylic acid tert-butyl ester (0.3 g, 1.01 mmoles) in anhydrous tetrahydrofuran (5 ml) was then added. The reaction mixture was stirred at -78 C. for 3 hours, quenched with saturated aqueous ammonium chloride, and partitioned between ethyl acetate and saturated aqueous ammonium chloride solution. The organic phase was washed with brine, dried over anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. The residue was purified by silica gel chromatography (10 to 45% ethyl acetate in hexane) to yield 3-[(7-Fluoro-benzo[b]thiophen-2-yl)-hydroxy-methyl]-3-(tetrahydro-pyran-4-ylmethyl)-pyrrolidine-1-carboxylic acid tert-butyl ester as a colorless semisolid (0.138 g, 30%). MS=450 [M+H]+., 346592-74-3

346592-74-3 7-Fluorobenzo[b]thiophene 21866059, abenzothiophene compound, is more and more widely used in various fields.

Reference£º
Patent; Roche Palo Alto LLC; US2009/318493; (2009); A1;,
Benzothiophene – Wikipedia
Benzothiophene | C8H6S – PubChem

5381-20-4, Thianaphthene-3-carboxaldehyde is a benzothiophene compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,5381-20-4

A mixture of thianaphthene-3-carboxaldehyde (0.2 g, 1.23 mmol), acetylacetone (0.25 mL, 2.47 mmol) and aqueous ammonium hydroxide solution (38-40%, 0.12 mL) in ethanol (1 mL) was heated to 90C and left to stir for 16 hours. The mixture was allowed to cool to RT and was then poured into 10 ml of cold water. The precipitate formed was filtered off, dried and washed with cold diethyl ether. The desired product was obtained as a strongly yellow solid (0.193 g, 48 %). 1H-NMR (400 MHz, DMSO-d6) delta = 2.17 (s, 6H), 2.29 (s, 6H), 5.52 (s, 1H), 7.23 (s, 1H), 7.33 (dt 2H), 7.88 (d, 1H), 8.12 (d, 1H), 9.08 (s, 1H). HPLC-MS: Rt 3.668 min, m/z 192.1 (MH+-134). The following examples were synthesized according to Method G.

As the paragraph descriping shows that 5381-20-4 is playing an increasingly important role.

Reference£º
Patent; Oncostellae, S.L.; KURZ, Guido; CAMACHO GOMEZ, Juan; (123 pag.)EP3480201; (2019); A1;,
Benzothiophene – Wikipedia
Benzothiophene | C8H6S – PubChem