Category: 149809-43-8

Related Products of 149809-43-8, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.149809-43-8, Name is ((3R,5R)-5-((1H-1,2,4-Triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate, molecular formula is C21H21F2N3O4S. In a Patent£¬once mentioned of 149809-43-8

PROCESS FOR PREPARATION OF POSACONAZOLE AND CRYSTALLINE POLYMORPHIC FORM V OF POSACONAZOLE

The present invention generally relates to a process for the preparation of an antifungal agent posaconazole and to a novel polymorphic form V of antifungal agent posaconazole.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 149809-43-8, and how the biochemistry of the body works.Related Products of 149809-43-8

Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 149809-43-8, name is ((3R,5R)-5-((1H-1,2,4-Triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate, introducing its new discovery. category: Tetrahydrofurans

Method for preparing high-purity posaconazole (by machine translation)

The invention discloses a method for preparation of posaconazole, first of all, BP004b04 with oxalic acid to form the salt, to obtain the POE; secondly, POE with di-tert-butyl b carbon ester in the presence of an alkali reaction to obtain POP, POP recrystallization; once again, with the POK POP in the presence of an alkali reaction to obtain the POR, POR removes uncle butyl carbonate protecting group, to obtain POS; finally POS POB ring obtained, with the POB POA reaction posaconazole. The method of the invention, obtained in the posaconazole, the diastereoisomeric isomer content ? 0.01%, and the whole route total yield is high. (by machine translation)

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 149809-43-8, and how the biochemistry of the body works.category: Tetrahydrofurans

Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Application of 149809-43-8, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 149809-43-8, molcular formula is C21H21F2N3O4S, introducing its new discovery.

A PROCESS FOR THE MANUFACTURE OF POSACONAZOLE

The present invention discloses an improved process for the manufacture of Posaconazole, an anti-fungal agent belonging to the category of substituted Tetrahydrofuran Triazole compound. The present invention further describes preparation of formula A and formula B, the key intermediates in the preparation of Posaconazole. The invention also discloses novel intermediates that are useful in the synthesis of Posaconazole.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 149809-43-8 is helpful to your research. Application of 149809-43-8

Reference£º
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.149809-43-8,((3R,5R)-5-((1H-1,2,4-Triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate,as a common compound, the synthetic route is as follows.

100 mL three-neck flask was added 2-[(1S,2S)-1-ethyl-2-benzyloxypropyl]-2,4-dihydro-4-[4-[4-(4-hydroxyphenyl)-1-piperazinyl]phenyl]-3H-1,2,4-triazol-3-one (formula III) (6.08 g) and DMSO (30 mL) were dissolved with stirring. A 25% aqueous solution of sodium hydroxide (1.7 mL) was added and the mixture was stirred for 15 min. Add (5R)-5-(2,4-difluorophenyl)-5-(1H-1,2,4-triazol-1-yl)methyltetrahydrofuran-3-ylmethyl 4-methylbenzenesulfonate (formula IV) (6.12 g), the mixture is stirred at 40-50 C for 12-18 h. The reaction mixture was poured into water (60 mL) with vigorous stirring, stirring vigorously for 30 min, suction filtration, the filter cake was washed with water (30 mL), and dried under vacuum at 50 C to obtain 8.83 g of the compound of formula (V), yield 95.6 %., 149809-43-8

149809-43-8 ((3R,5R)-5-((1H-1,2,4-Triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate 10895629, aTetrahydrofurans compound, is more and more widely used in various fields.

Reference£º
Patent; Kunming Jida Pharmaceutical Co., Ltd.; Yang Zhuqi; Zhang Poyong; Sun Xiaomei; Wang Lijiang; Zhang Yun; (13 pag.)CN108239077; (2018); A;,
Tetrahydrofuran – Wikipedia
Tetrahydrofuran | (CH2)3CH2O – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.149809-43-8,((3R,5R)-5-((1H-1,2,4-Triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate,as a common compound, the synthetic route is as follows.

To a solution of intermediate (Xla) (7.80 g, 25.1 mmol) in DMSO (60 mL) was added aq sodium hydroxide (3.0 mL, 12.5 M, 37.6 mmol). The mixture was stirred at RT for 10 min and was then treated portionwise with ((3S,5 )-5-((1 /-/-1 ,2,4-triazol-1-yl)methyl)-5-(2,4-difluoro phenyl)tetrahydrofuran-3-yl)methyl4-methylbenzenesulfonate (IX) (ex APIChem, Catalogue Number: AC-8330, 12.4 g, 27.6 mmol). The reaction mixture was stirred at 30C for 18 hr, cooled to RT and water (200 mL) was added. The resulting mixture was extracted with EtOAc (3 x 200 mL) and the combined organic extracts were washed with brine (2 x 200 mL), and then dried and evaporated in vacuo to afford a brown oil. Analysis of the crude, Boc-protected product (Vila) by 1 H NMR indicated that it contained -10% of the alkene: ( )-1-((2-(2,4- difluorophenyl)-4-methylenetetrahydrofuran-2-yl)methyl)-1 /-/-1 ,2,4-triazole, formed as an elimination by-product. The crude urethane (Vila) was taken up into DCM (150 mL) and treated with TFA (39.0 mL, 502 mmol). After 2 hr at RT the reaction mixture was concentrated in vacuo to remove most of the volatiles and was then diluted with EtOAc (200 mL) and washed with aq. NaOH (2 M, 200 mL). The aq phase was separated and was extracted with EtOAc (2 x 200 mL). The combined organic extracts were washed with brine (2 x 200 mL) and then dried and evaporated in vacuo to afford a light brown oil. The crude product was purified by flash column chromatography (Si02, 80 g, 0-10% 0.7 M NH3/MeOH in DCM, gradient elution) to afford the title compound, intermediate (V), as a viscous, light brown oil (9.46 g, 80%); R’ 1.91 min (Method b); m/z 470 (M+H)+ (ES+); 1 H NMR delta: 2.07 (3H, s), 2.15 (1 H, dd), 2.36-2.42 (1 H, m), 2.52-2.56 (1 H, m), 2.79-2.81 (4H, m), 2.87-2.90 (4H, m), 3.66 (1 H, dd), 3.73-3.77 (2H, m), 4.04 (1 H, t), 4.57 (2H, dd), 6.64 (1 H, dd), 6.70-6.75 (2H, m), 6.99 (1 H, td), 7.25-7.34 (2H, m), 7.76 (1 H, s) and 8.34 (1 H, s)., 149809-43-8

As the paragraph descriping shows that 149809-43-8 is playing an increasingly important role.

Reference£º
Patent; PULMOCIDE LIMITED; SUNOSE, Mihiro; COLLEY, Thomas Christopher; ITO, Kazuhiro; RAPEPORT, Garth; STRONG, Peter; (55 pag.)WO2016/87878; (2016); A1;,
Tetrahydrofuran – Wikipedia
Tetrahydrofuran | (CH2)3CH2O – PubChem

149809-43-8, ((3R,5R)-5-((1H-1,2,4-Triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate is a Tetrahydrofurans compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Example -3: Preparation of 4-(4-(4-(4-(((3R,5R)-5-((lH-l,2,4-triazol-l-yl)methyl)-5- (2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-l-yl)phenyl)-l- ((2S,3S)-2-(benzyloxy)pentan-3-yl)-lH-l,2,4-triazol-5(4H)-one of the structural formula (III) of crystalline Form B-3 l-((2S,3S)-2-(benzyloxy)pentan-3-yl)-4-(4-(4-(4-hydroxyphenyl)piperazin-l-yl)phenyl)- lH-l,2,4-triazol-5(4H)-one (4.0 Kg, 1.0 eq.) of the structural formula (II) was dissolved in Dimethyl sulfoxide (6.0 vol.) at 25¡À2C under nitrogen and cooled to 15-20 C. 25% aqueous sodium hydroxide solution (1.3 eq.) was added to the reaction mixture and was stirred for 10 minutes. ((3S,5R)-5-((lH-l,2,4-triazol-l-yl)methyl)-5-(2,4- difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate of the structural formula (I) (4.02 Kg) was added to the reaction mixture and continued to stir for lh at 15- 20 C. Reaction temperature was raised to 28¡À2C and stirred for 45-50 h. Ethyl acetate (5.0 vol.) was added to the reaction mass and cooled to 15-20 C followed by addition of water (5.0 vol.), reaction mass was slowly warmed to 25¡À2C and stirred. Layers were separated; organic layer was collected. Aqueous layer was again extracted with Ethyl acetate (3 vol.). Combined organic layers were washed with water (3 vol.) and organic layer was concentrated partially to contain 5.0 Vol. of Ethyl acetate. Cooled the partially concentrated solution to 25¡À2C and was added n-Heptane (5.0 vol.), stirred at 28¡À2C for 30 min and further diluted with n- Heptane (2.0 vol.) heated to 42¡À2C, stirred for 30 min and then slowly cooled to 28¡À2C and continue to stir at 28¡À2C for 2h. The above mixture was cooled to 0-5 C and stirred for lh. Solid was filtered; washed with Heptane (5 vol.). Dried under VTD at 60+5 C to yield 4-(4-(4-(4-(((3R,5R)-5-((lH-l,2,4-triazol- 1 -yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methoxy)phenyl)piperazin- 1 – yl)phenyl)-l-((2S,3S)-2-(benzyloxy)pentan-3-yl)-lH-l,2,4-triazol-5(4H)-one of the structural formula (III) of crystalline Form B-3 with 96% yield. Characteristic Physico-Chemical Data of Crystalline Form B-3 of the Compound of Structural Formula III Physical appearance: Off-white to white solid X-ray Powder Diffraction Pattern: See Figure 3 and Table 3 DSC: See Figure 4 IR: See Figure 5

149809-43-8, The synthetic route of 149809-43-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; BIOCON LIMITED; CHARYULU, Palle, Venkata, Raghavendra; GOWDA, Dharshan, Jakkali, Chandre; RAJMAHENDRA, Shanmughasamy; RAMAN, Manikandan; (41 pag.)WO2017/51342; (2017); A1;,
Tetrahydrofuran – Wikipedia
Tetrahydrofuran | (CH2)3CH2O – PubChem

149809-43-8, ((3R,5R)-5-((1H-1,2,4-Triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate is a Tetrahydrofurans compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a solution of intermediate (Vlllb) (100 g, 271 mmol) in DMF (500 ml_) under a nitrogen atmosphere was added sodium ethoxide (22.2 g, 325 mmol) resulting in a mild exotherm (from 20 to 22.0C). After stirring at 15-25C for 45 min the reaction mixture was treated with the tosylate (IX) (146.4 g, 325 mmol) and was then heated at 60-65C for 2 hr. Analysis of the resulting mixture by HPLC indicated that the reaction was essentially complete (4.4% phenol remaining, 14.6% tosylate, 77.6% product) and the mixture was cooled to 40-45C and I PA (800 ml_) was added. Water was then added drop-wise at 40-45C until a slight haze persisted (required 500 ml_) at which point a small sample of the product (100 mg, 0.15 mmol) was added as a seed and the mixture stirred for 10 min at 40-45C to ensure precipitation was initiated. Water (500 ml_) was added drop-wise at 40-45C and the suspension then cooled to 15-25C. The resulting solid was collected by filtration, washed with water (3 x 200 ml_) and then dried in vacuo at 50C give the crude product as an off-white solid (155.9 g, 89%, HPLC purity 94.8%). A portion of this material (85.0 g) was taken up in IPA (510 ml_) by heating at 65-75C until dissolution was complete. The solution was then cooled to 15-25C and stirred for 30 min. The resulting solid was collected by filtration, washed with IPA (2 x 85 ml_) and dried in vacuo at 50C to give the title compound, intermediate (IVc) as a white solid (83.4g, 87% overall yield, HPLC purity 98.2%); R< 15.74 min; m/z 646.6 (M+H)+ (ES+), 149809-43-8

149809-43-8 ((3R,5R)-5-((1H-1,2,4-Triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate 10895629, aTetrahydrofurans compound, is more and more widely used in various fields.

Reference£º
Patent; PULMOCIDE LIMITED; SUNOSE, Mihiro; COLLEY, Thomas Christopher; ITO, Kazuhiro; RAPEPORT, Garth; STRONG, Peter; (55 pag.)WO2016/87878; (2016); A1;,
Tetrahydrofuran – Wikipedia
Tetrahydrofuran | (CH2)3CH2O – PubChem

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.149809-43-8,((3R,5R)-5-((1H-1,2,4-Triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate,as a common compound, the synthetic route is as follows.

EXAMPLE 2PREPARATION OF BENZYL POSACONAZOLE OF FORMULA (Ila); In a clean, dry round bottomed flask 23 ml of dimethylsulfoxide and 4.74 gm of compound of formula (III) were charged at room temperature and stirred for about 15 minutes. Previously prepared NaOH solution (0.53 gm of NaOH dissolved in 3.74 ml of water) was added into the flask at about room temperature and stirred for about 30 minutes. 5 gm of compound of formula (IVa) was added to the reaction solution and stirred at about 35C to about 40C for about 12 hours. After completion of the reaction, the reaction solution was cooled to about 0C and 50 ml of water was added dropwise and stirred for about 30 minutes. The formed precipitate was filtered and washed with 80 ml of water. The solid was dried in air oven at about 45C to about 50C to yield 6.6 gm of the title compound. Purity by HPLC: 92%, 149809-43-8

The synthetic route of 149809-43-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; GLENMARK GENERICS LIMITED; GHARPURE, Milind; KRISHNA, Vivek; SANIKOMMU, Srinivas Reddy; CHAUDHARI, Ganesh; VERDIA, Jitendra; KHAN, Mubeen Ahmed; WO2011/158248; (2011); A2;,
Tetrahydrofuran – Wikipedia
Tetrahydrofuran | (CH2)3CH2O – PubChem

149809-43-8, ((3R,5R)-5-((1H-1,2,4-Triazol-1-yl)methyl)-5-(2,4-difluorophenyl)tetrahydrofuran-3-yl)methyl 4-methylbenzenesulfonate is a Tetrahydrofurans compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated,149809-43-8

To a solution of 4-bromo-2-methyl phenol (920 mg, 4.89 mmol) in DMSO (10 mL) was added aq sodium hydroxide (0.39 mL, 12.5 M, 4.89 mmol) and the mixture stirred at RT for 10 min and then treated with the tosylate (IX) (2.00 g, 4.45 mmol). The reaction mixture was stirred at 60C for 72 hr then cooled to RT and partitioned between water (25 mL) and EtOAc (20 mL). The organic phase was separated and retained and the aq layer was extracted with EtOAc (3 x 25 mL). The combined organic extracts were washed with brine (3 x 15 mL) and then dried and evaporated in vacuo. The crude product was purified by flash column chromatography (S1O2, 12 g, 0-30% EtOAc in DCM, gradient elution) to give the title compound, intermediate (XIII), as a colourless oil (1.84 g, 86%); Rl 2.78 min (Method a); m/z 464 (M+H)+ (ES+); 1 H NMR delta: 2.09 (3H, s), 2.17 (1 H, dd), 2.37-2.43 (1 H, m), 2.52-2.60 (1 H, m), 3.72-3.78 (2H, m), 3.82 (1 H, dd), 4.00-4.06 (1 H, m), 4.57 (2H, dd), 6.82 (1 H, d), 7.00 (1 H, td), 7.25-7.34 (4H, m), 7.76 (1 H, s), 8.34 (1 H, s).

The synthetic route of 149809-43-8 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PULMOCIDE LIMITED; SUNOSE, Mihiro; COLLEY, Thomas Christopher; ITO, Kazuhiro; RAPEPORT, Garth; STRONG, Peter; (55 pag.)WO2016/87878; (2016); A1;,
Tetrahydrofuran – Wikipedia
Tetrahydrofuran | (CH2)3CH2O – PubChem