Category: 1172623-99-2

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.1172623-99-2, Name is tert-Butyl ((2R,3S)-2-(2,5-difluorophenyl)-5-hydroxytetrahydro-2H-pyran-3-yl)carbamate, molecular formula is C16H21F2NO4. In a Article，once mentioned of 1172623-99-2, Computed Properties of C16H21F2NO4

A series of new phenylpropenamide derivatives containing different substituents was synthesized, characterized and evaluated for their anti-hepatitis B virus (HBV) activities. The quantitative structure eactivity relationships (QSAR) of phenylpropenamide compound have been studied. The 2D-QSAR models, based on DFT and multiple linear regression analysis methods, revealed that higher values of total energy (TE) and lower entropy (Stheta) enhanced the anti-HBV activities of the phenylpropenamide molecules. Predictive 3D-QSAR models were established using SYBYL multifit molecular alignment rule. The optimum models were all statistically significant with cross-validated and conventional coefficients, indicating that they were reliable enough for activity prediction.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.HPLC of Formula: C16H21F2NO4, you can also check out more blogs about1172623-99-2

Reference：
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.

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, 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; 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

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.

1H (11.53 g, 35.03 mmol) was dissolved in dichloromethane (130 mL), cooled to 0 C A dess martin oxidant (29.72 g, 70.06 mmol)Was added to the reaction solution in portions and allowed to stand at room temperature for 4 hours.The solution was cooled to 0 C, saturated sodium bicarbonate solution (60 mL) was added dropwise to the reaction mixture, stirred for 20 minutes, filtered, the filtrate was allowed to stand,The aqueous phase was extracted with methyl tertiary butyl ether (60 mL x 3) and the combined organic phases were washed with saturated sodium bicarbonate solution (30 mL x 2). The organic phase was dried over anhydrous sodium sulfate,(10.85 g, yield 94.7%) as a white crystalline powder, and the residue was purified by column chromatography (petroleum ether / ethyl acetate (v / v) = 10: 1-4: 1).

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; FAN, JIANG; CHEN, QINGPING; JIANG, WEI; ZHENG, SUXIN; YE, FEI; (128 pag.)TW2017/8221; (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

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

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

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

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.

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

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) and cooled to 0 C.Dess-Martin periodinane (29.72 g, 70.06 mmol) was added portionwise to the reaction mixture and allowed to react to room temperature for 4 hours. Cool down to 0 C,Saturated sodium hydrogen carbonate solution (60 mL) was added dropwise to the reaction mixture, stirred for 20 minutes, and filtered.The filtrate was allowed to stand for stratification, and the aqueous phase was extracted with methyl tert-butyl ether (60 mL ¡Á 3).Wash with saturated sodium bicarbonate solution (30 mL ¡Á 2), dry over anhydrous sodium sulfate, and then concentrated by filtration and eluted by column chromatography ( petroleum ether / ethyl acetate (v/v) = 10:1-4:1 ),The white crystalline powder Intermediate 1 (10.85 g, yield 94.7%) was obtained.

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; Sichuan Hai Sike Pharmaceutical Co., Ltd.; Fan Jiang; Feng Jianchuan; Peng Fei; Chen Qingping; (45 pag.)CN105085530; (2019); B;,
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 6: Ru Oxidation to Provide 9; To a solution of the alcohol 8 (40.0 g, 121.4 mmol) in CH3CN (120 mL), AcOH (20 mL), and H2O (20 mL) was added a solution of RuCl3 (50.4 mg, 0.243 mmol) in H2O (40 mL) at 0 C. NaBrO3 (9.2 g, 60.7 mmol) was added in portions at 0 C. The resulting reaction mixture was stirred at 0 C. until a complete consumption of alcohol 8 was achieved by HPLC. H2O (600 mL) was added dropwise over 5 h at 0 C. The slurry was aged overnight at 0 C. The product was collected by filtration, washed with CH3CN/H2O=1/9 (200 mL¡Á2), and dried under vacuum to give 9. 9 has two rotomers in DMSO in about a 4:1 ratio at ambient temperature. For the major rotomer of 9: 1H NMR (500 MHz, DMSO-d6): delta 7.27 (m, 1H), 7.20 (m, 2H), 7.12 (d, J=9.2 Hz, 1H), 4.76 (d, J=9.5 Hz, 1H), 4.19 (d, J=16.1H), 4.10 (d, J=16.1 z, 1H), 4.05 (m, 1H), 2.76 (dd, J=16.4, 6.2 Hz, 1H), 2.71 (dd, J=16.4, 10.1 Hz, 1H), 1.20 (s, 9H). 13C-NMR (125 MHz, d6-DMSO): delta 205.4, 158.0 (d, J=236.9 Hz), 156.2 (dd, J=241.8, 1.8 Hz), 154.2, 127.8 (dd, J=16.0, 8.0 Hz), 116.6 (dd, J=25.2, 8.0 Hz), 116.2 (dd, J=23.4, 8.0 Hz), 115.2 (dd, J=24.0, 3.1 Hz), 77.9, 74.5, 73.6, 50.6, 44.1, 27.9., 1172623-99-2

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

Reference£º
Patent; Xu, Feng; Kim, Mary M.; Kohmura, Yoshinori; Sladicka, Tricia; Rosen, Jonathan D.; Zacuto, Michael J.; US2009/187028; (2009); 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.

1H (11.53 g, 35.03 mmol) was dissolved in dichloromethane (130 mL) Cooling to 0C ,Dess-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 0C ,Saturated sodium bicarbonate solution (60 mL) was added dropwise to the reaction solution, stirred for 20 minutes,The organic phase was washed with saturated sodium bicarbonate solution (30 mL x 2), and the organic phase was dried over anhydrous sodium sulfate and dried over anhydrous sodium sulfate (60 mL x 3). The organic phase was washed with saturated sodium bicarbonate solution (30 mL x 2) , Filtered and concentrated by 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%). (30 mL x 2), and the solvent was concentrated to give a white solid, 1H (7.9 g, 84% yield).

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.; FAN, JIANG; ZHANG, CHEN; PENG, FEI; WU, YE; FENG, JIANCHUAN; WANG, JIANMIN; ZHENG, SUXIN; WEI, YONGGANG; YE, FEI; (350 pag.)TW2017/8220; (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.

A solution of 1 Hg (11.53 g, 35.03 mmol)Was dissolved in dichloromethane (130 mL) and cooled to 0 C. Dess-Martin periodinane (29.72 g, 70.06 mmol) was added portionwise to the reaction solution and allowed to warm to room temperature for 4 hours The Down to 0 C,The saturated sodium bicarbonate solution (60mL) was added dropwise to the reaction solution, stirred for 20 minutes, filtered, the filtrate was allowed to stand and the aqueous phase was extracted with methyl tertiary butyl ether (60 mL chi 3) (30 mL chi 2). The organic phase was dried over anhydrous sodium sulfate, filtered and concentrated. Column chromatography (petroleum ether / ethyl acetate (nu / nu) = 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; FAN, JIANG; FENG, JIAN-CHUAN; PENG, FEI; CHEN, QING-PING; (89 pag.)TW2017/8224; (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

Ruthenium chloride (45 mg) was added to a solution oftert-butyl[(2R,3S)-5-hydroxy-2-(2,5-difluorophenyl)tetrahydro-2H-pyran-3-yl]carbamate (15.0 g; Formula IX;Example 10) and acetic acid (15.0 mL) in acetonitrile (45.0 mL) and water (7.5 mL) at0C. Sodium bromate (4.0 g) was added slowly to the reaction mixture at 0C to 5C overS hours, and then the mixture was stirred for 16 hours at -5C to 5C. After completion ofthe reaction, IPA (15 mL) was added over 25 minutes at 0C to 5C, and then the mixture was stirred for 15 minutes. Water (180 mL) was slowly added to the reaction mixture, and then the mixture was stirred for 5 hours at 0C to 5C. The reaction mixture was filtered, and then dried under reduced pressure at 45C to 50C to obtain the title compound.Yield: 80%, 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; SUN PHARMACEUTICAL INDUSTRIES LIMITED; PANDYA, Bhargav; THAKUR, Mandeep; SURADKAR, Swapnil; ANGADI, Surender; (42 pag.)WO2017/81590; (2017); A1;,
Tetrahydropyran – Wikipedia
Tetrahydropyran – an overview | ScienceDirect Topics