Category: 1172623-99-2

Electric Literature of 1172623-99-2. Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 1172623-99-2, Name is tert-Butyl ((2R,3S)-2-(2,5-difluorophenyl)-5-hydroxytetrahydro-2H-pyran-3-yl)carbamate

Phenylpropenamide derivatives: Anti-hepatitis B virus activity of the Z isomer, SAR and the search for novel analogs

Phenylpropenamides have been reported to be a class of non-nucleoside inhibitors of the hepatitis B virus (HBV). This class of compounds was explored with the objective of developing potent anti-HBV agents, with a novel mechanism of action, that could be combined with nucleos(t)ide analogs currently used to treat HBV infection. To accomplish this objective a series of substituted arylpropenamide derivatives were prepared and the E and Z geometrical isomers were separated. The structural identity of each of the E and Z isomers was determined by single crystal X-ray crystallography. Contrary to previous reports, the activity of this class of molecules resides in the Z isomer. Further structure-activity relationship studies around the active Z isomer identified compounds that displayed potent antiviral activity against HBV with EC90 value of approximately 0.5 muM in vitro. Attempts to develop ring constrained analogs did not lead to active HBV inhibitors.

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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.

Tert-butyl (2R,3S)-2-(2,5-difluorophenyl)-5-hydroxyltetrahydro-2H-pyran-3-ylcarbamate (2.33 g, 7.08 mmol) was dissolved in a mixed solution of 24 mL acetonitrile, 4 mL water and 4 mL acetic acid. Thereto was added an aqueous solution (4 mL) of ruthenium chloride hydrate (3.7 mg, 0.0142 mmol), and cooled to 0 C. Sodium bromate (535 mg, 3.54 mmol) was added, and stirred at low temperature for about 1.5 hours until the raw materials were completely reacted. To the reaction solution was added 120 mL water, stirred at 0 C overnight, and extracted with dichloromethane. The organic phase was washed with water, dried and concentrated, and then the residue was purified by silica gel column chromatography (petroleum ether/ethyl acetate, 10:1) to give the intermediate 1 tert-butyl (2R,3S)-2-(2,5-difluorophenyl)-5-oxotetrahydro-2H-pyran-3-ylcarbamate (1.71 g) as a white solid in 74% yield. 1H-NMR (400 MHz, CDCl3): delta=7.22(1H, m), 7.00(1H, m), 4.82 (1H, m), 4.63 (1H, m), 4.29(1H, d, J=16.2Hz), 4.11(1H, d, J=16.4Hz), 4.05 (1H, m), 3.05(1H, m), 2.85 (1H, m), 1.30 (9H, s).

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; Centaurus BioPharma Co., Ltd.; Chai Tai Tianqing Pharmaceutical Group Co., Ltd.; Lianyungang Runzhong Pharmaceutical Co., Ltd.; XU, Xinhe; SHEN, Yu; XIAO, Dengming; LUO, Hong; PENG, Yong; HAN, Yongxin; ZHANG, Aiming; YANG, Ling; (51 pag.)EP3257857; (2017); A1;,
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

Step O: tert-Butyl [(2R,3S)-2-(2,5-difluorophenyl)-5-oxotetrahydro-2H-pyran-3-yl]carbamate To 46.8 kg (142 mol) of tert-butyl [(2R,3S)-2-(2,5-difluorophenyl)-5-hydroxytetrahydro-2H-pyran-3-yl]carbamate in a stirred vessel was added acetonitrile (150 kg), acetic acid (50 kg), and water (25 kg). After dissolving at room temperature, the solution was cooled to 0 C. and RuCl3.3H2O (250 g, 956 mmol) in water (50 kg) was added under nitrogen. Then, NaBrO3 (11.7 kg, 77.5 mol) was added in six portions every 1.5 h under nitrogen. After stirring at 0 C. for 6 h, 2-propanol (31 kg) was added over 30 min. at 0 C. Then, water (720 kg) was added at this temperature over 5 h. The resulting slurry was stirred overnight, filtered, and cake washed with water. The solids were then dried under vacuum at 40-60 C. to give tert-butyl [(2R,3S)-2-(2,5-difluorophenyl)-5-oxotetrahydro-2H-pyran-3-yl]carbamate., 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; Merck Sharp & Dohme Corp; Merck Sharp & Dohme Ltd.; Arroyo, Itzia Z.; Krueger, Davida; Chen, Ping; Moment, Aaron J.; Biftu, Tesfaye; Sheen, Faye; Zhang, Yanfeng; US9181262; (2015); B2;,
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)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.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