Category: 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.

General procedure: To a solution of 3-nitro- 4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)benzenesulfonamide (63 mg, 0.20 mmol) in DCM (20 mL) was added EDC*HC1 (58 mg, 0.30 mmol) followed by DMAP (49 mg, 0.40 mmol) at 0 C. After 10 min, Intermediate 26 (140 mg, 0.20 mmol) and N- methylmorpholine (0.07 mL, 0.60 mmol) were added and the reaction was warmed to rt. After 16 h, water was added, and the mixture was extracted with DCM. The combined organic layers were dried over Na2S04, filtered and concentrated. The crude product was purified by HPLC (10:90 to 99: 1 lOmM NH4C03H(aq.)/ CH3CN) to afford Example 1 (69 mg, 39%) as a yellow solid. NMR (300 MHz, DMSO -d6) d 11.68 (br s, 1H), 11.42 (br s, 1H), 8.58 (br s, 1H), 8.53 (s, 1H), 8.03 (d, 7=2.1 Hz, 1H), 7.77 (d, 7=8.4 Hz, 1H), 7.54-7.46 (m, 3H), 7.10-7.02 (m, 1H), 6.74-6.68 (m, 1H), 6.38 (s, 1H), 6.25 (s, 1H), 3.89-3.82 (m, 2H), 3.33-3.22 (m, 4H), 3.19-3.05 (m, 4H), 2.90 (s, 2H), 2.33 (br s, 4H), 2.29 (s, 6H), 2.05-1.95 (m, 2H), 1.95-1.82 (m, 1H), 1.69-1.57 (m, 4H), 1.32-1.18 (m, 4H), 0.82 (s, 6H).; LC/MS (ESI) m/z 858.4 [M+H]+., 1228779-96-1

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

Reference£º
Patent; ZENO ROYALTIES & MILESTONES, LLC; PINCHMAN, Joseph, Robert; HUANG, Peter, Qinhua; BUNKER, Kevin, Duane; SIT, Rakesh, Kumar; SAMATAR, Ahmed, Abdi; (236 pag.)WO2019/139902; (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

EXAMPLE 27H4- {4-[(4′-chloro-l , 1 ‘-biphenyl-2-yl)methyl]-3-isobutylpiperazin-l -yl} -N-( {3-nitro-4- [(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-phenoxybenzamide; EXAMPLE 27G (13 mg), EXAMPLE IF (7 mg), l-ethyl-3-[3- (dimethylamino)propyl]-carbodiimide hydrochloride (8 mg), and 4-dimethylaminopyridine (5 mg) were stirred in CH2Cl2 (1 mL) for 24 hours. The product was purified by preparative HPLC using a Cl 8 column, 250 x 50 mm, lOmu, and eluting with a gradient of 20-100% CH3CN vs. 0.1% trifluoroacetic aicd in water, giving the product as a trifluoroacetate salt. 1H NMR (300 MHz, dimethylsulfoxide-d6) delta 11.62 (br s, IH), 9.10 (br s, IH), 8.65 (t, IH), 8.47 (d, IH), 7.77 (dd, IH), 7.70 (br s, IH), 7.50 (m, 5H), 7.39 (m, 3H), 7.25 (m, 2H), 7.18 (d, IH), 7.01 (dd, IH), 6.83 (m, 2H), 6.76 (m, IH), 6.40 (br s, IH), 4.70 and 4.15 (both v br s, total IH), 3.85 (dd, 2H), 3.60 (v br s, IH), 3.32, 3.27, 3.24, 3.06 (all m, total 1 IH), 1.90 (m, IH), 1.62 (m, 3H), 1.30 (m, 4H), 0.70 (br m, 6H)., 1228779-96-1

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

Reference£º
Patent; ABBOTT LABORATORIES; BRUNCKO, Milan; DING, Hong; DOHERTY, George, A.; ELMORE, Steven, W.; HASVOLD, Lisa; HEXAMER, Laura; KUNZER, Aaron, R.; MANTEI, Robert, A.; MCCLELLAN, William, J.; PARK, Chang, H.; PARK, Cheol-min; PETROS, Andrew, M.; SONG, Xiaohong; SOUERS, Andrew, J.; SULLIVAN, Gerard, M.; TAO, Zhi-fu; WANG, Gary, T.; WANG, Le; WANG, Xilu; WENDT, Michael, D.; WO2010/65865; (2010); A2;,
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.,1228779-96-1

A 3-L jacketed reactor (Kettle 1) equipped with a mechanical stirrer, nitrogen inlet/outlet, temperature control unit and reflux condenser was inerted with nitrogen and charged with 3-nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)benzenesulfonamide (19.7 g, 0.95 equiv), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC, 22.1 g, 1.75 equiv), 4-dimethylaminopyridine (DMAP, 16.1 g, 2 equiv) and dichloromethane (DCM, 200 ml_, 5 vo I). In a separate 1-L reactor (Kettle 2) equipped with a mechanical stirrer, nitrogen inlet/outlet was charged with 2-((1 H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4′-chloro-5,5- dimethyl-3, 4, 5, 6-tetrahydro-[1 ,1 ‘-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid hydrochloride salt (40.0 g, 65.8 mmol), and DCM (400 mL, 10 vol). Triethylamine (36.7 mL, 4.00 equiv) was added in one portion. The solution in Kettle 2 was dosed into Kettle 1 using a transfer pump. The batch was stirred at room temperature for 5-25 h then acetic acid (10% v/v, 10 Vol, 400 mL) was added to the batch and stirred for 15 min.

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

Reference£º
Patent; ALBANY MOLECULAR RESEARCH, INC.; GREGG, Brian, Thomas; GEISS, William, Bert; HERR, Robert, Jason; RAI, Ravi, R; (39 pag.)WO2020/23435; (2020); A1;,
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.,1228779-96-1

Compound 16-2 was dissolved in dichloromethane,Add (3eq) EDCI, (0.3eq) DMAPAfter 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 30:1 gave compound S16.

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

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.

Compound 6-2 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 30:1 gave compound S6.

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 fields.

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.

In a 100-mL flask (flask I) 2-[(1H-Pyrrolo[2,3-b]pyridine-5-yl)oxy]-4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl]methyl]piperazin-1-yl]benzoic acid sulfate salt (compound 2a) (assay: 14.88 mmol), Et3N (12 mL, 87.5 mmol) and dichloromethane (85 mL) were combined at 20-25C and stirred for complete dissolution. In a 250-mL three necked round bottom flask (flask II) equipped with magnetic stirrer, thermometer, 3-nitro-4-[[(tetrahydropyran-4-yl)methyl]amino]-benzenesulfonamide (4.60 g, 14.58 mmol), DMAP (7.12 g, 58.34 mmol), N,N-diisopropylcarbodiimide (6 mL, 38.5 mmol) and dichloromethane (106 mL) were combined and stirred for 15 minutes. The resulting acid solution (flask I) was slowly added to the suspension of the sulfonamide (flask II) within 1 hour and reaction mixture agitated at 35-40C until reaction completion. The reaction mixture was extracted with 10% aqueous acetic acid (2×57 mL), 5% aqueous NaHCO3 (57 mL) and 5% aqueous NaCl (57 mL). After phase separation the organic layer was evaporated. Yield: 55%

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 fields.

Reference£º
Patent; ASSIA CHEMICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; POTARINE JUHASZ, Zsuzsa; STRUBA, Szabolcs; NEMETHNE RACZ, Csilla; TOTH, Zoltan Gabor; SZILAGYI, Andrea; KERTI-FERENCZI, Renata; MOLNAR, Sandor Janos; PASZTOR-DEBRECZENI, Nora; HAJKO, Janos; (100 pag.)WO2017/156398; (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,1228779-96-1

General procedure: To a solution of appropriate crude acid (1 eq) in CH2Cl2 wereadded EDCI (3 eq), DMAP (0.3 eq) and DIPEA (3 eq). The solutionwas stirred at room temperature for 0.5 h and compound 23 [7] (0.8eq) was added. The resulting mixture was stirred for another 8 hand water was added. The layers were separated, and the aqueouslayer was extracted with CH2Cl2. The combined organic layer waswashed with brine, dried over anhydrous Na2SO4, filtered, andconcentrated under vacuo. The residue was prified by chromatography(CH2Cl2/CH3OH 40:1) to provide target compounds 27a-i,28a-d and 34a-c.

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

Reference£º
Article; Liu, Xiaohua; Zhang, Yu; Huang, Wenjing; Luo, Jia; Li, Yang; Tan, Wenfu; Zhang, Ao; European Journal of Medicinal Chemistry; vol. 159; (2018); p. 149 – 165;,
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.

EXAMPLE 1 J (3.39 g), EXAMPLE 2A (1.87 g), l-ethyl-3-[3-(dimethylamino)propyl]- carbodiimide hydrochloride (2.39 g), and 4-dimethylaminopyridine (1.09 g) were stirred in CH2C12 (40 mL) for 24 hours. The residue was purified by flash chromatography, eluting with 25-100%o ethyl acetate in hexanes, then 10% methanol in ethyl acetate with 1% acetic acid to give the product as a white solid. .H NMR (300MHz, dimethylsulfoxide-d6) 11.65 (brs, 1H), 8.55 (br s, 1H), 8.04 (d, 1H), 7.89 (dd, 1H), 7.51 (m, 3H), 7.33 (d, 2H), 7.08 (m, 1H), 7.04 (d, 2H), 6.68 (dd, 1H), 6.39 (d, 1H), 6.19 (d, 1H), 3.84 (m, 1H), 3.30 (m, 4H), 3.07 (m, 4H), 2.73(m, 2H), 2.18 (m, 6H), 1.95 (m, 2H), 1.61 (dd, 2H), 1.38 (m, 2H), 1.24 (m, 4H), 0.92 (s, 6H)., 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; ABBOTT LABORATORIES; TAO, Zhi-Fu; WANG, Xilu; SOUERS, Andrew J.; CATRON, Nathaniel D.; SULLIVAN, Gerard; WO2011/150016; (2011); 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 8-mL round-bottom flask, was placed 4-(4- [[2-(4-chlorophenyl)-4,4-dimethylcyclohex- i-en-i – ylj methyljpiperazin- 1 -yl)-2- [ i4-thia-2,4, iO-triazatricyclo [7.5 .0.0?[3 ,7j jtetradeca- 1 (9),2,5,7- tetraen-iO-yljbenzoic acid (30 mg, 0.05 mmol, 1 equiv), 3-nitro-4-[[(oxan-4- yl)methyljaminojbenzene-i-sulfonamide (17 mg, 0.06 mmol, 1.20 equiv), EDCI (18 mg, 0.09 mmol, 2 equiv), DMAP (23 mg, 0.19 mmol, 4 equiv), DCM (3 mL). The resulting solution was stirred for overnight at room temperature. The resulting mixture was concentrated. The crude product was purified by Flash-Prep-HPLC with the following conditions (IntelFlash-i): Column, Ci8 silica gel; mobile phase, Water(0.i%FA) and ACN (48.0% ACN up to 53.0% in 7 mm, hold 95.0% in 1 mm, down to 48.0% in 1 mm within 5 ; Detector, UV 254 nm. This resulted in 10.6 mg (24.15%) of 4-(4- [[2-(4-chlorophenyl)-4,4-dimethylcyclohex- i-en-i – ylj methyljpiperazin- 1 -yl)-N-(3 -nitro-4- [[(oxan-4-yl)methylj aminoj benzenesulfonyl)-2- [1 4-thia- 2,4, iO-triazatricyclo [7.5 .0.0?[3 ,7jjtetradeca- 1 (9),2,5,7-tetraen- iO-yljbenzamide as a yellow solid. LC-MS: (ES, m/z): M+i=939, R,T= 3.55 mm. The measurements of the retention were done with a reversed phase column (C 18). Shimadzu LCMS 2020; 50*3.0 Kinetex 2.6u XB-Ci8 2.6 microm; Eluent A: water (0.05 % TFA); Eluent B: Acetonitrile; linear gradient. H-NMR:(CDC13, 300ppm): 8.7i(s, iH), 8.49 (s, iH), 7.99-7.97(m, iH), 7.8i-7.77(m, iH), 7.38-7.28(m,4H), 7.Oi-6.93(m, 2H), 6.88-6.72(m, 3H), 3.36(s, iH), 4.06-3.26(m, i8H), 2.73-2.22(m, 6H),2.i3-i.73(m, 3H), i.79-i.25(m, 6H), i.00(s, 6H)., 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 fields.

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

The a mixture of 3- ((1H-pyrrolo [2, 3-b] pyridin-5-yl) oxy) -4′- ((S)-2-(2-cyclopropylphenyl) pyrrolidin-1-yl) -2′, 3′, 4′, 5′-tetrahydro- [1, 1′-biphenyl] -4-carboxylic acid (650 mg, 1.25 mmol) in DCM (20 mL) was added EDCI (480 mg, 2.50 mmol), triethylamine (630 mg, 6.26 mmol), 3-nitro-4- (((tetrahydro-2H-pyran-4-yl) methyl) amino) benzenesulfonamide (395 mg, 1.25 mmol) and DMAP (306 mg, 2.50 mmol), the solution was stirred at r.t for 40 h. The reaction solution was washed with H 2O (30 mL3), concentrated and purified by chromatography column on silica (eluent: MeOH/DCM = 0/25 to 1/25) to afford the product (700 mg, 68.5%). MS (ESI, m/e) [M+1] + 817.2. 1H NMR (400 MHz, DMSO-d 6) delta ppm: 11.64 (s, 1H), 8.48 (s, 2H), 7.96 (s, 1H), 7.80-7.40 (m, 5H), 7.30-6.84 (m, 5H), 6.73 (s, 1H), 6.35 (s, 1H), 6.04-5.79 (m, 1H), 3.88-3.81 (m, 2H), 3.32-3.16 (m, 6H), 2.38-1.21 (m, 18H), 0.97-0.84 (m, 2H), 0.72-0.50 (m, 2H). MS (ESI) m/e [M+1] + 763.2. MS (ESI) m/e [M+1] + 805.2

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