Tag: M.W:300-400

1172623-99-2, tert-Butyl ((2R,3S)-2-(2,5-difluorophenyl)-5-hydroxytetrahydro-2H-pyran-3-yl)carbamate is a Tetrahydropyrans compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1H (11.53 g, 35.03 mmol) was dissolved in dichloromethane (130 mL)Cooling to 0 ,The Dayton Martin oxidant (29.72 g, 70.06 mmol) was added portionwise to the reaction solution,Naturally rose to room temperature for 4 hours.Cooling to 0 ,The saturated sodium bicarbonate solution (60 mL) was added dropwise to the reaction solution,Stir for 20 minutes,filter,The filtrate was allowed to stand,The aqueous phase was extracted with methyl tert-butyl ether (60 mL x 3)Combined organic phase,The organic phase was washed with saturated sodium bicarbonate solution (30 mL x 2)Dried over anhydrous sodium sulfate,Filter concentrate,The residue was purified by silica gel column chromatography (petroleum ether / ethyl acetate (v / v) = 10: 1-4: 1)To give white crystalline powder intermediate 1 (10.85 g, yield 94.7%)., 1172623-99-2

As the paragraph descriping shows that 1172623-99-2 is playing an increasingly important role.

Reference£º
Patent; Sichuan Hai Sike Pharmaceutical Co., Ltd.; Fan Jiang; Chen Qingping; Wang Chengtao; (36 pag.)CN106632349; (2017); A;,
Tetrahydropyran – Wikipedia
Tetrahydropyran – an overview | ScienceDirect Topics

1172623-99-2, tert-Butyl ((2R,3S)-2-(2,5-difluorophenyl)-5-hydroxytetrahydro-2H-pyran-3-yl)carbamate is a Tetrahydropyrans compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Oxalyl chloride (0.295g, 2.28mmol) was added to dichloromethane (20mL), the system was cooled to -70 deg.] C, dimethylsulfoxide (0.18g, 2.28mmol) was slowly added to the above solution, maintaining the temperature of the system – 70 stirring continued for 10 minutes, N-Boc- (2R, 3S) -2- (2,5- difluorophenyl) -5-hydroxy-tetrahydro -2H- pyran-3-amine (0.5g, 1.52mmol ) in dichloromethane (10 mL) was slowly added to the solution, and then slowly added triethylamine (0.46g, 4.56mmol), the resulting solution was incubated for 30 minutes, warmed to room temperature and the reaction was continued for 30 minutes and dichloromethane (30 mL ) was poured into the reaction mixture, washed with saturated sodium bicarbonate solution was added the other (20 mL), brine.The organic layer was concentrated to dryness and the residue was purified by silica gel column chromatography: to give a white solid (0.38 g, purity 97.6%, yield: 76.1%) (eluent ethyl acetate, n-hexane)., 1172623-99-2

The synthetic route of 1172623-99-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Shenzhen Han Yu Pharmaceutical Co., Ltd; Liu, Feipeng; Mi, Pengcheng; Tao, Anjin; Ma, Yaping; Yuan, Jiancheng; (18 pag.)CN106316888; (2017); 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.,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.,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.

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

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.

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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1172623-99-2,tert-Butyl ((2R,3S)-2-(2,5-difluorophenyl)-5-hydroxytetrahydro-2H-pyran-3-yl)carbamate,as a common compound, the synthetic route is as follows.

Oxalyl chloride (0.295g, 2.28mmol) was added to dichloromethane (20mL), the system was cooled to -70 deg.] C, dimethylsulfoxide (0.18g, 2.28mmol) was slowly added to the above solution, maintaining the temperature of the system – 70 stirring continued for 10 minutes, N-Boc- (2R, 3S) -2- (2,5- difluorophenyl) -5-hydroxy-tetrahydro -2H- pyran-3-amine (0.5g, 1.52mmol ) in dichloromethane (10 mL) was slowly added to the solution, and then slowly added triethylamine (0.46g, 4.56mmol), the resulting solution was incubated for 30 minutes, warmed to room temperature and the reaction was continued for 30 minutes and dichloromethane (30 mL ) was poured into the reaction mixture, washed with saturated sodium bicarbonate solution was added the other (20 mL), brine.The organic layer was concentrated to dryness and the residue was purified by silica gel column chromatography: to give a white solid (0.38 g, purity 97.6%, yield: 76.1%) (eluent ethyl acetate, n-hexane)., 1172623-99-2

1172623-99-2 tert-Butyl ((2R,3S)-2-(2,5-difluorophenyl)-5-hydroxytetrahydro-2H-pyran-3-yl)carbamate 86713019, aTetrahydropyrans compound, is more and more widely used in various fields.

Reference£º
Patent; Shenzhen Han Yu Pharmaceutical Co., Ltd; Liu, Feipeng; Mi, Pengcheng; Tao, Anjin; Ma, Yaping; Yuan, Jiancheng; (18 pag.)CN106316888; (2017); A;,
Tetrahydropyran – Wikipedia
Tetrahydropyran – an overview | ScienceDirect Topics

1172623-99-2, tert-Butyl ((2R,3S)-2-(2,5-difluorophenyl)-5-hydroxytetrahydro-2H-pyran-3-yl)carbamate is a Tetrahydropyrans compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

1H (11.53 g, 35.03 mmol) was dissolved in dichloromethane (130 mL)Slow down to 0 C, will be wearing a Dess Martin oxidizer(29.72 g, 70.06 mmol) was added portionwise to the reaction solution,Naturally rose to room temperature for 4 hours.After cooling to 0 C, saturated sodium bicarbonate solution (60 mL) was added dropwise to the reaction solution, stirred for 20 minutes, filtered, the filtrate was allowed to stand for separation, and the aqueous phase was extracted with methyl tertiary butyl ether (60 mL x 3) The organic phase was combined and the organic phase was washed with saturated sodium bicarbonate solution (30 mL x 2), dried over anhydrous sodium sulfate and concentrated by filtration. The residue was purified by silica gel column chromatography (petroleum ether / ethyl acetate (v / v) = 10 : 1-4: 1) to give white crystalline powder intermediate 1 (10.85 g, yield 94.7%).

1172623-99-2, As the paragraph descriping shows that 1172623-99-2 is playing an increasingly important role.

Reference£º
Patent; SICHUAN HAISCO PHARMACEUTICAL CO., LTD; ZHANG, CHEN; FAN, JIANG; LEI, MING; WEI, YONG-GANG; (61 pag.)TW2017/8223; (2017); A;,
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