Tag: 1228779-96-1

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1228779-96-1,3-Nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)benzenesulfonamide,as a common compound, the synthetic route is as follows.

A mixture of 2- ((1H-pyrrolo [2, 3-b] pyridin-5-yl) oxy)-4-(4-oxocyclohexyl) benzoic acid (2.0g, 5.71mmol), 3-nitro-4- (((tetrahydro-2H-pyran-4-yl) methyl) amino) benzene sulfonamide (1.8 g, 5.71 mmol), EDCI (1.64 g, 8.57 mmol), DMAP (1.05 g, 8.57 mmol) and TEA (1.15 g, 16.42 mmol) in DCM (20 mL) was stirred at ambient temperature for 20 hours. The reaction mixture was concentrated in vacuum, then purified by chromatography column on silica (eluent: DCM/MeOH = 100/1 to 50/1) to afford 2- ((1H-pyrrolo [2, 3-b] pyridin-5-yl) oxy) -N- ((3- nitro-4- (((tetrahydro-2H-pyran-4-yl) methyl) amino) phenyl) sulfonyl)-4-(4-oxocyclohexyl) benzamide (1.5 g). MS (ESI) m/e [M+1] + 648.1.

1228779-96-1, The synthetic route of 1228779-96-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BEIGENE, LTD.; GUO, Yunhang; XUE, Hai; WANG, Zhiwei; SUN, Hanzi; (493 pag.)WO2019/210828; (2019); A1;,
Tetrahydropyran – Wikipedia
Tetrahydropyran – an overview | ScienceDirect Topics

1228779-96-1, 3-Nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)benzenesulfonamide is a Tetrahydropyrans compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 2- ((1H-pyrrolo [2, 3-b] pyridin-5-yl) oxy)-4-(6- (2-phenylpyrrolidin-1-yl) pyridin-3-yl) benzoic acid (150 mg, 0.32 mmol) in dichloromethane (25 mL) were added o- (7-azabenzotriazol-1-yl) -N, N, N’, N’-tetramethyluronium hexafluorophosphate (182 mg, 0.48 mmol), triethylamine (1 mL) and 4-Dimethylaminopyridine (40 mg, 0.32 mmol). The mixture was stirred for 0.5 h at r.t. Then 3-nitro-4- (((tetrahydro-2H-pyran-4-yl) methyl) amino) benzenesulfonamide (199 mg, 0.64 mmol) was added. The reaction was continually stirred overnight at r.t. Afterwards, the mixture was washed with water (15 mL) and the organic layers were dried over anhydrous Na 2SO 4 and concentrated. The residue was further purified by prep-HPLC to give the product (40 mg, 16.2 %). 1H NMR (400 MHz, DMSO-d 6) delta ppm: 12.25 (s, 1H), 11.69 (s, 1H), 8.61 (s, 1H), 8.56 (d, J = 2.0 Hz, 1H), 8.25 (s, 1H), 8.03 (d, J = 2.0 Hz, 1H), 7.82 (d, J = 7.3 Hz, 1H), 7.68-7.46 (m, 4H), 7.38 (d, J = 8.2 Hz, 1H), 7.27 (t, J = 7.3 Hz, 2H), 7.22-7.07 (m, 4H), 6.97 (s, 1H), 6.38 (s, 1H), 6.30 (d, J = 8.2 Hz, 1H), 5.05 (d, J = 7.1Hz, 1H), 3.83 (t, J = 10.0 Hz, 3H), 3.57 (d, J = 9.3 Hz, 1H), 3.31-3.18 (m, 4H), 2.42-2.27 (m, 1H), 1.88-1.78 (m, 4H), 1.60 (d, J = 12.2 Hz, 2H), 1.31-1.14 (m, 2H). MS (ESI, m/e) [M+1] + 774.1

1228779-96-1, 1228779-96-1 3-Nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)benzenesulfonamide 57474953, aTetrahydropyrans compound, is more and more widely used in various.

Reference£º
Patent; BEIGENE, LTD.; GUO, Yunhang; XUE, Hai; WANG, Zhiwei; SUN, Hanzi; (493 pag.)WO2019/210828; (2019); A1;,
Tetrahydropyran – Wikipedia
Tetrahydropyran – an overview | ScienceDirect Topics

1228779-96-1, 3-Nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)benzenesulfonamide is a Tetrahydropyrans compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

3-nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino )benzenesulfonamide ( 4.73 g) wasdissolved m dichloromethane (124.8 mL) at 34C. 1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (3.66 g) and 4-Dimethylaminopyridine(3.33 g) was added to the above solution and stirred for 10 minutes at 35C. A mixture of2-( ( 1H -pyrrolo [2,3-b ]pyridin-5-yl)oxy)-4-( 4-( ( 4′-chloro-5,5-dimethy 1-3,4,5 ,6-tetrahydro[1,1′-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid (7.8 g), triethylamine (3.8 g) indichloromethane (70.2 mL) was stirred for 15 minutes at 35C and it was added dropwise to the above mixture in 15 minutes at the same temperature. The reaction mixturewas stirred for 23 hours at 31 oc and then evaporated the solvent from the reactionmixture to obtain residue. This residue was dissolved in ethyl acetate (80 mL) and washedthe solution with 10% acetic acid (2×80 mL), saturated aqueous sodium bicarbonatesolution (2×80 mL) and then with brine solution (2×80 mL). The separated organic layerwas dried over sodium sulfate and evaporated the solvent completely. The crude productwas combined with acetonitrile (112 mL) and stirred for 2 hour at 34C and filtered thesolid. The solid was dissolved in acetonitrile (60 mL) at 70C and stirred for 1 hour at thesame temperature. The solution was cooled and filtered the solid to obtain titlecompound. Yield: 4.5 g; Purity by HPLC: 99.65%, 1228779-96-1

1228779-96-1 3-Nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)benzenesulfonamide 57474953, aTetrahydropyrans compound, is more and more widely used in various.

Reference£º
Patent; DR. REDDY?S LABORATORIES LIMITED; PEDDIREDDY, Subba Reddy; KOTTUR, Mohan Kumar; JURUPULA, Ramprasad; BAIG, Mohammed Azeezulla; CHAKKA, Ramesh; THIPPARABOINA, Rajesh; PEDDY, Vishweshwar; RAO, Pallavi; ORUGANTI, Srinivas; DAHANUKAR, Vilas Hareshwar; (88 pag.)WO2017/212431; (2017); A1;,
Tetrahydropyran – Wikipedia
Tetrahydropyran – an overview | ScienceDirect Topics

1228779-96-1, 3-Nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)benzenesulfonamide is a Tetrahydropyrans compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Into a 40-mL round-bottom flask, was placed 4-(4- ((4?-chloro-5 ,5-dimethyl-3 ,4,5,6-tetrahydro- [1,1 ?-biphenylj -2-yl)methyl)piperazin- 1 -yl) -2-(3 – methoxy-3 ,4-dthydro-2H-pyrrolo [3?,2?:5,6 jpyrido [2,3-bj [1 ,4joxazepin- 1 (7H)-yl)benzoic acid (50 mg, 0.08 mmol, 1 equiv), DCM (3 mL), 3-nitro-4-[[(oxan-4-yl)methyljaminojbenzene-1- sulfonamide (25.2 mg, 0.08 mmol, 1.00 equiv), EDCI (30.6 mg, 0.16 mmol, 2 equiv), DMAP (39.0 mg, 0.32 mmol, 4 equiv). The resulting solution was stirred for overnight at 25 degrees C. The resulting mixture was concentrated under vacuum. The residue was applied onto a silica gel column with dichloromethane/methanol(10:1). The crude product was purified by Flash-PrepHPLC with the following conditions (IntelFlash-1): Column, C18 reversed phase column; mobile phase, Water (1OMMOL/L NH4HCO3+0.05%NH3.H20) and CH3CN (20.0% CH3CN up to 90.0% in 30 mm); Detector, UV 220 nm. This resulted in 32 mg (40.0%) of 4-(4-((4?-chloro- 5 ,5-dimethyl-3 ,4,5,6-tetrahydro- [1,1 ?-biphenylj -2-yl)methyl)piperazin- 1 -yl) -2-(3 -methoxy-3 ,4- dthydro-2H-pyrrolo [3?,2?:5,6 jpyrido [2,3-bj [1 ,4 joxazepin- 1 (7H)-yl)-N-((3-nitro-4-(((tetrahydro- 2H-pyran-4-yl)methyl)amino)phenyl)sulfonyl)benzamide as a yellow solid. LC-MS: (ES, m/z):M+1=953, R,T= 3.44 mm. ?H NMR (300 MHz, DMSO-d6 ppm) 11.00 (ds, 1H), 8.56 (s, 2H), 7.47-7.44 (m, 2H), 7.36-7.33 (m, 2H), 7.08-7.04 (m, 3H), 6.78-6..65 (m, 2H), 6.57-6.54 (m, 1H),6.43 (s, 1H), 6.04 (s, 1H), 4.05-3.15 (m, 20H), 3.13 (s, 1H), 2.70-2.35 (m, 4H), 2.03 (s, 3H),1.92-1.90 (m, 1H), 1.89-1.87 (m, 2H), 1.7 1-1.67 (m, 2H), 1.53-1.45 (m, 3H), 0.97 (s, 6H)., 1228779-96-1

As the paragraph descriping shows that 1228779-96-1 is playing an increasingly important role.

Reference£º
Patent; NEWAVE PHARMACEUTICAL INC.; CHEN, Yi; LOU, Yan; (108 pag.)WO2019/40550; (2019); A1;,
Tetrahydropyran – Wikipedia
Tetrahydropyran – an overview | ScienceDirect Topics

1228779-96-1, 3-Nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)benzenesulfonamide is a Tetrahydropyrans compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of 2- ((1H-pyrrolo [2, 3-b] pyridin-5-yl) oxy)-4-(5- (2-phenylpyrrolidin-1-yl) pyrazolo [1, 5-a] pyrimidin-2-yl) benzoic acid (250 mg, 0.484 mmol), 3-nitro-4- (((tetrahydro-2H-pyran-4-yl) methyl) amino) benzenesulfonamide (150 mg, 0.484 mmol), EDCI (196 mg, 0.969 mmol), DMAP (88 mg, 0.727 mmol) and TEA (150 mg, 1.452 mol) in DCM (10 ml) was stirred at ambient temperature for 4 d. The reaction solution was washed with H 2O (10 mL), concentrated, purified by column chromatograph on silica gel (100-200 mesh, eluted with DCM: MeOH = 20: 1) to give a crude product, the crude product was purified by pre-HPLC to give the product (80 mg). 1H NMR (DMSO-d 6) delta ppm: 12.35 (s, 1H), 11.79 (s, 1H), 8.69-8.31 (m, 3H), 8.09 (d, J = 2.4 Hz, 1H), 7.87 (dd, J = 9.2, 2.4 Hz, 1H), 7.77-7.50 (m, 4H), 7.31-7.15 (m, 7H), 6.50-6.43 (m, 2H), 5.15 (s, 1H), 3.89-3.82 (m, 3H), 3.64 (s, 1H), 3.30-3.21 (m, 5H), 2.39-2.33 (m, 1H), 1.93-1.82 (m, 4H), 1.59 (d, J = 12.0 Hz, 2H), 1.29-1.18 (m, 2H). MS (ESI, m/e) [M+1] + 814.1.

The synthetic route of 1228779-96-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BEIGENE, LTD.; GUO, Yunhang; XUE, Hai; WANG, Zhiwei; SUN, Hanzi; (493 pag.)WO2019/210828; (2019); A1;,
Tetrahydropyran – Wikipedia
Tetrahydropyran – an overview | ScienceDirect Topics

1228779-96-1, 3-Nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)benzenesulfonamide is a Tetrahydropyrans compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of 2-(lH-pyrrolo[2,3-b]pyridin-5-yloxy)-4-(4-((2-(4- chlorophenyl)-4,4-dimethylcyclohex- 1 -enyl)methyl)piperazin- 1 -yl)benzoic acid( 16g,28mmol) and 3-nitro-4-((tetrahydro-2H-pyran-4-yl)methylamino)benzenesulfonamide(8.83g, 28mmol) in DCM(300mL) was added EDCI(10.74g, 56mmol) and DMAP(6.85g, 56mmol). The mixture was stirred at r.t. overnight. LC/MS showed the expected product as a single peak. The mixture was diluted with DCM(500ml) and washed with aq. NaHC03, water, brine and dried over Na2S04. The residue after evaporation of solvent was dissolved in DCM and loaded on a column and eluted with 30% ethyl acetate in DCM followed by 1 to 2% MeOH in DCM to give 24.5g pure product(95% purity) which was dissolved in DMSO and MeOH(l :l) and TFA(2eq) and loaded on a 330g C18 column (6g a time)to give 13.5g pure(>99.7% purity) product(55%yield). The API was extracted using dichloromethane and then, the solvent was removed using rotary evaporator. The resulting solid was suspended in acetonitrile at ambient temperatures to reach its solubility. After equilibrating, the solids were isolated at ambient temperature.

1228779-96-1 3-Nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)benzenesulfonamide 57474953, aTetrahydropyrans compound, is more and more widely used in various.

Reference£º
Patent; ABBOTT LABORATORIES; CATRON, Nathaniel D.; CHEN, Shuang; GONG, Yuchuan; ZHANG, Geoff G.; WO2012/71336; (2012); A1;,
Tetrahydropyran – Wikipedia
Tetrahydropyran – an overview | ScienceDirect Topics

1228779-96-1, 3-Nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)benzenesulfonamide is a Tetrahydropyrans compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound 4-3 was dissolved in dichloromethane,Add (3 eq) EDCI, (0.3 eq) DMAP,After stirring at room temperature for half an hour, compound 1-5 (0.8 eq) was added.It is then reacted at room temperature for 6-8 hours. After the reaction is completed, the reaction is quenched with water.Extract three times with dichloromethane, and combine the organic phases with saturated brine.After drying anhydrous sodium sulfate, mix the sample on the column.CH2Cl2: MeOH = 100:1 to 40:1 gave compound S4.

The synthetic route of 1228779-96-1 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Chinese Academy Of Sciences Shanghai Pharmaceutical Institute; Zhang Ao; Tan Wenfu; Liu Xiaohua; Huang Wenjing; Zhang Yu; Yang Jun; (37 pag.)CN110143974; (2019); A;,
Tetrahydropyran – Wikipedia
Tetrahydropyran – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1228779-96-1,3-Nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)benzenesulfonamide,as a common compound, the synthetic route is as follows.

(0074) Compound 1E (115 mg), Compound 1F (67 mg), 1-ethyl-3-[3-(dimethylamino)propyl]carbodiimide hydrochloride (82 mg), and 4-dimethylaminopyridine (26 mg) were stirred in CH2Cl2 (3 ml) for 24 hours. The reaction was cooled and chromatographed on silica gel with 0-5% methanol/ethyl acetate. 1H NMR (300 MHz, dimethylsulfoxide-d6) delta 11.48 (brs, 1H), 8.34 (br s, 1H), 8.31 (m, 1H), 7.90 (d, 1H), 7.68 (m, 1H), 7.58 (m, 2H), 7.46 (m, 4H), 7.35 (m, 2H), 7.21 (dd, 1H), 6.76 (m, 4H), 6.28 (m, 2H), 3.02 (m, 2H), 2.89 (m, 4H), 2.80 (m, 4H), 2.40 (m, 3H), 1.59 (m, 2H), 1.25 (m, 4H), 0.87 (m, 2H).

1228779-96-1 3-Nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)benzenesulfonamide 57474953, aTetrahydropyrans compound, is more and more widely used in various.

Reference£º
Patent; AbbVie Inc.; Catron, Nathaniel; Lindley, David; Miller, Jonathan M.; Schmitt, Eric A.; Tong, Ping; US10213433; (2019); B2;,
Tetrahydropyran – Wikipedia
Tetrahydropyran – an overview | ScienceDirect Topics

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1228779-96-1,3-Nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)benzenesulfonamide,as a common compound, the synthetic route is as follows.

The mixture of 3- ((1H-pyrrolo [2, 3-b] pyridin-5-yl) oxy) -4′- (2- (2-cyclopropylphenyl) pyrrolidin-1-yl) -2′, 3′, 4′, 5′-tetrahydro- [1, 1′-biphenyl] -4-carboxylic acid (700 mg, 1.34 mmol), triethylamine (106 mg, 4.05 mmol), 2- (7-azabenzotriazol-1-yl) -N, N, N’, N’-tetramethyluronium hexafluorophosphate (616 mg, 1.62 mmol) in DCM (10 mL) was stirred for 2 hours at room temperature. To the reaction mixture was added 3-nitro-4- (((tetrahydro-2H-pyran-4-yl) methyl) amino) benzenesulfonamide (512 mg, 1.62 mmol) and DMAP (17 mg, 0.14 mmol) and stirred overnight. The reaction mixture was washed with brine, dried over Na 2SO 4 and concentrated in vacuo, then purified by chromatography column on silica (eluent: DCM/MeOH = 50/1 to 15/1) to afford a crude product (490 mg). The crude product was purified with Pre-HPLC to give the product (1.65 mg, 1.26%). 1H NMR (400 MHz, DMSO-d 6) delta ppm: 12.25 (br, 1H), 11.68 (br, 1H), 8.51 (m, 2H), 7.99 (s, 1H), 7.79 (d, J = 12.0 Hz, 1H), 7.61-7.47 (m, 4H), 7.28-7.07 (m, 5H), 6.73 (s, 1H), 6.37 (s, 1H), 5.99-5.85 (m, 1H), 5.32-5.28 (m, 1H), 3.85 (d, J = 8.0 Hz, 2H), 3.75-3.51 (m, 2H), 3.22 (m, 5H), 2.42-1.97 (m, 8H), 1.86 (s, 2H), 1.73 (s, 1H), 1.61-1.57 (m, 2H), 1.45-1.37 (m, 1H), 1.23 (m, 2H), 1.07-0.93 (m, 2H), 0.71-0.59 (m, 2H). MS (ESI, m/e) [M+1] + 817.2.

As the paragraph descriping shows that 1228779-96-1 is playing an increasingly important role.

Reference£º
Patent; BEIGENE, LTD.; GUO, Yunhang; XUE, Hai; WANG, Zhiwei; SUN, Hanzi; (493 pag.)WO2019/210828; (2019); A1;,
Tetrahydropyran – Wikipedia
Tetrahydropyran – an overview | ScienceDirect Topics