Tag: M.W=0-100

Electric Literature of 3279-95-6, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 3279-95-6, name is 2-(Aminooxy)ethanol, molecular formula is C2H7NO2, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.

Starting from intermediate 1.i (0.103 g; 0.2 mmol) and 2-aminooxyethanol (0.017 g; 0.221 mmol), the solutionwas stirred for th. The reaction mixture was directly purified by prep-HPLC (Method 1) to afford the titlecompound (0.084 g, 86% yield) as a white amorphous solid.MS1 (ESI, m/z): 485.1 [M+H*] for CigH2aN4O7So; tr = 0.65 min.

According to the analysis of related databases, 3279-95-6, the application of this compound in the production field has become more and more popular.

Reference:
Patent; IDORSIA PHARMACEUTICALS LTD; DIETHELM, Stefan; MATHIEU, Gaelle; PANCHAUD, Philippe; SURIVET, Jean-Philippe; TIDTEN-LUKSCH, Naomi; (123 pag.)WO2019/38362; (2019); A1;,
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Reference of 3513-81-3, In the chemical reaction process,reaction time,type of solvent,can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product.An updated downstream synthesis route of 3513-81-3 as follows.

2-METHYLENE-1, 3-propanediol (2.20 g, 25.0 MM) was stirred in dichloromethane (20 ML) and cooled to 0 °C. A 1 N solution of diethylzinc in hexanes (3.40 g, 27.5 MM) was added followed by a solution OF 4-BROMO-3-FLUORO-N-HYDROXYBENZENECARBOXIMIDOYL chloride (6.30 g, 25.0 MM) in dichloromethane (40 mL). The reaction was allowed to warm to room temperature and was complete after four hours. The solution was diluted with ammonium chloride and extracted using dichloromethane. The organic layer was dried (magnesium sulfate), filtered and concentrated to give the desired product as a yellow solid (4.72 g). MS (ESP : 305 (MH+) for CLLHLLBREINO3 300 MHz NMR (DMSO-D 6 : 3.29 (s, 2H); 3.55 (s, 2H); 3.57 (s, 2H) ; 5.10 (t, 2H); 7.52 (d, 1H); 7.68 (d, 1H); 7.86 (t, 1H).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,3513-81-3, its application will become more common.

Reference:
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2004/48392; (2004); A1;,
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Reference of 14320-38-8, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.14320-38-8, name is Cyclopent-3-enol, molecular formula is C5H8O, molecular weight is 84.12, as common compound, the synthetic route is as follows.

To a solution of cyclopent-3-en-1-ol (compound 32a, 5.0 g, 59.4 mmol) in THF (100.0 ml) was added NaH (3.1 g, 77.2 mmol) in portions at 0 oC. The reaction was stirred at the same temperature for 30 minutes, then BnBr (10.2 g, 59.4 mmol) was added dropwise. The reaction was warmed to room temperature and stirred for 12 hours. The reaction was quenched with H2O (300 mL) and extracted with EtOAc twice (200 mL). The combined organic layer was dried over Na2SO4, concentrated to give compound 32b (12.5 g, crude) as a brown oil.

Statistics shows that 14320-38-8 is playing an increasingly important role. we look forward to future research findings about Cyclopent-3-enol.

Reference:
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; HU, Taishan; KOU, Buyu; LIN, Xianfeng; LIU, Haixia; ZHANG, Zhisen; (152 pag.)WO2018/11160; (2018); A1;,
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Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 1072-52-2, name is 2-(Aziridin-1-yl)ethanol. This compound has unique chemical properties. The synthetic route is as follows. category: alcohols-buliding-blocks

Example 4 (Table 1, entry 2, and Scheme 6): Preparation 2-[2-(aminocarbonyl)(2- chloroethyl)-4,6-dinitroanilino] ethyl methanesulfonate (13a); A solution of 2-chloro-3,5- dinitrobenzamide (11) (250 mg, 1.15 mmol) in THF (20 mL) was cooled to below 5 0C, and aziridineethanol (240 mg, 2.76 mmol) was added over 10 min to the stirred mixture, which was then kept at 20 0C overnight. Water (50 mL) was added, followed by EtOAc (50 mL). The mixture was separated and aqueous phase was extracted with EtOAc (2×60 mL). The combined organic fractions were washed with brine, dried and concentrated under reduced pressure, chromatography on silica gel and elution with EtOAc/petroleum ether (1:1), to give 2-[(2-chloroethyl)(2-hydroxyethyl)amino]-3,5-dinitrobenzamide (12a) (350 mg, 92%) as a yellow solid: mp (EtOAc/petroleum ether) 96-100 C; 1H NMR [(CD3)2SO] delta 8.69 (d, / = 2.8 Hz, 1 H), 8.43 (s, 1 H, CONH), 8.35 (dj = 2.8 Hz, 1 H), 8.10 (s, 1 H), 5.15 (tj = 5.6 Hz, 1 H), 3.77 (m, 2 H), 3.54 (m, 4 H), 3.14 (m, 2 H); 13C NMR delta 167.6, 146.7, 143.8, 139.7, 134.1, 128.2, 123.1, 57.8, 54.3, 53.6, 41.4; Anal. Calcd. for C11H13ClN4O6: C, 39.7; H, 3.9, N, 16.8. Found: C, 38.4; H, 4.4; N, 15.7%.

If you are interested in these compounds, you can also browse my other articles.Thank you for taking the time to read this article. I hope you enjoyed it, 1072-52-2, 2-(Aziridin-1-yl)ethanol.

Reference:
Patent; AUCKLAND UNISERVICES LIMITED; WO2008/30112; (2008); A1;,
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Reference of 14320-38-8, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.14320-38-8, name is Cyclopent-3-enol, molecular formula is C5H8O, molecular weight is 84.12, as common compound, the synthetic route is as follows.

Cyclopent-3-en-l-ol (10 g, 118.9 mmol) was dissolved in DMF (100 mL) at 0 C, then lH-imidazole (17.29 mL, 261.5 mmol) was added followed by tert- butyl(chloro)dimethylsilane (21.5 g, 142.7 mmol) and warmed up to r.t.. The mixture was stirred at r.t. for 14 h, diluted with EtOAc (300 mL) and washed with 5 % LiCl (2x 100 mL), brine (50 mL), dried over sodium sulfate, filtered, and concentrated under reduced pressure. The crude residue was purified by flash column chromatography (Si02, 0-10% EtOAc in hexanes) to afford 17.2 g (73 %) of the title product as a colourless clear liquid. 1H NMR (250 MHz, CDC13) delta ppm 5.66 (s, 2H), 4.53 (tt, J 7.0, 3.6 Hz, 1H), 2.57 (dd, J 15.2, 6.8 Hz, 2H), 2.27 (dd, J 15.3, 3.6 Hz, 2H), 0.89 (s, 9H), 0.06 (s, 6H).

The chemical industry reduces the impact on the environment during synthesis 14320-38-8, I believe this compound will play a more active role in future production and life.

Reference:
Patent; UCB BIOPHARMA SPRL; ALEXANDER, Rikki, Peter; BRACE, Gareth, Neil; BROWN, Julien, Alistair; CALMIANO, Mark, Daniel; CHOVATIA, Praful, Tulshi; DELIGNY, Michael; GALLIMORE, Ellen, Olivia; HEER, Jag, Paul; JACKSON, Victoria, Elizabeth; KROEPLIEN, Boris; MAC COSS, Malcolm; QUINCEY, Joanna, Rachel; SABNIS, Yogesh, Anil; SWINNEN, Dominique, Louis, Leon; ZHU, Zhaoning; WO2015/86526; (2015); A1;,
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Electric Literature of 4415-82-1, Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps,and cheap raw materials. 4415-82-1, name is Cyclobutylmethanol. A new synthetic method of this compound is introduced below.

2-Cyclobutanecarbaldehyde Chemical Formula: C5HgO Exact Mass: 84.06 Molecular Weight: 84.12 To a mixture of Pyridinium chlorochromate (41.3 g, 191.6 mmol) in dichloromethane (120 mL) was added Cyclobutanemethanol (7.5 g, 87.1 mmol). The mixture was stirred for 1.5 hours then filtered through a pad of silica and rinsed with further dichloromethane (300 mL). The solvent was removed under reduced pressure to give 2-cyclobutylcarbaldehyde (10.0 g, contains residual dichloromethane) that was used without further purification.

At the same time, in my other blogs, there are other synthetic methods of this type of compound,4415-82-1, Cyclobutylmethanol, and friends who are interested can also refer to it.

Reference:
Patent; ALKERMES PHARMA IRELAND LIMITED; BLUMBERG, Laura, Cook; DEAVER, Dan; EYERMAN, David; WO2014/190270; (2014); A1;,
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Adding a certain compound to certain chemical reactions, such as: 124-68-5, 2-Amino-2-methyl-1-propanol, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound, Recommanded Product: 124-68-5, blongs to alcohols-buliding-blocks compound. Recommanded Product: 124-68-5

2-Amino-2-methyl-l-propanol (5 g, 56.1 mmol), (Boc)20 (13.46 g, 61.7 mmol) and triethyl amine (6.24 g, 61.7 mmol) were dissolved in 50 mL of dichloromethane. The reaction mixture was stirred for 4 h at 22 to 25 C. Above mixture was washed with water (25 mL x 2), dried over anhydrous sodium sulfate and concentrated under vacuum to get tert-buty] (1- hydroxy-2-methylpropan-2-yl)carbamate (10.3 g, 97% yield).

The synthetic route of 124-68-5 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; NEKTAR THERAPEUTICS (INDIA) PVT.LTD.; NEKTAR THERAPEUTICS (Incorporated under the Laws of Delaware and domiclled in the State of California); DUARTE, FRANCO; ANAND, NEEL; SHARMA, PANKAJ; SINGH, DEVENDRAPRATAP U.; WO2015/79459; (2015); A1;,
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Application of 2002-24-6, Adding some certain compound to certain chemical reactions, such as: 2002-24-6, name is 2-Aminoethanol hydrochloride,molecular formula is C2H8ClNO, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 2002-24-6.

Step A N-tritylethanolamine Ethanolamine hydrochloride (9.9 g; 100 mmol) is partially dissolved in CH2 Cl2 /CH3 CN (200 ml/100 ml) and Et3 N (23 ml; 170 mmol) is then added. Tritylchloride (18.9 g; 67.6 mmol) is added portionwise over 30 minutes. After the addition is complete the reaction mixture is allowed to stir an additional 30 minutes, diluted with CH2 Cl2, washed With H2 O 2* and brine, dried (MgSO4), concentrated in vacuo and purified by column chromatography with silica/CH2 Cl2 to give N-tritylethanolamine as an oil which is used directly in Step B.

According to the analysis of related databases, 2002-24-6, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Rhone-Poulenc Rorer Pharmaceuticals Inc.; US5455260; (1995); A;,
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Adding a certain compound to certain chemical reactions, such as: 16545-68-9, Cyclopropanol, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound, Formula: C3H6O, blongs to alcohols-buliding-blocks compound. Formula: C3H6O

A mixture of 2-bromo-6-fluoropyridine (371 mg, 2.1 mmol) and cyclopropanol (350 mg, 6.0 mmol) in NMP (6 mL) was stirred for 5 minutes at 0 oC. Then to the solution was added dropwise a solution of t-BuOK in THF (1M, 0.6 mL, 0.6 mmol) at 0 oC. After addition, the reaction mixture was warmed to RT and stirred for 2 h. The reaction mixture was poured into a mixed solvent of PE/EA/water (50 mL/50mL/100 mL). The organic layer was separated, washed with 5% of LiCl aqueous solution (20 mL), dried over anhydrous Na2SO4, and filtered. The filtrate was concentrated in vacuo, and the residue was purified by silica gel column (5% ~ 10% EA/PE) to afford 2-bromo-6-cyclopropoxypyridine (374 mg, 83%) as a colorless oil. LC- MS m/z: 216&218 [M+H]+. Purity (214 nm): 99.6%.

The synthetic route of 16545-68-9 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; LYSOSOMAL THERAPEUTICS INC.; SKERLJ, Renato, T.; BOURQUE, Elyse Marie Josee; LANSBURY, Peter, T.; GREENLEE, William, J.; GOOD, Andrew, C.; (309 pag.)WO2017/176961; (2017); A1;,
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Application of 627-27-0 ,Some common heterocyclic compound, 627-27-0, molecular formula is C4H8O, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.

Intermediate 38. [0131] NaH (50% in oil, 2.88 g, 0.06 mol) was slowly added to a solution of Intermediate 37 (3 g, 0.041 mol) in 30 mL anhydrous DMF in ice-bath. After stirring for 0.5 h, BnBr (5.38 mL, 0.045 mol) was added to the reaction solution and stirred at r.t. for overnight. The mixture was poured into 80 mL H2O at 0 C., extracted with EtOAc. The combined organic phase was washed with aq. NH4Cl, brine and dried over Na2SO4. After concentration, the residue was dissolved in PE (petroleum ether), and filtered through a pad of silica gel. The filtrate was concentrated to afford the Intermediate 38 as colorless oil.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,627-27-0, its application will become more common.

Reference:
Patent; MICURX PHARMACEUTICALS, INC.; GORDEEV, Mikhail Fedorovich; LIU, Jinqian; YUAN, Zhengyu; WANG, Xinghai; US2013/165411; (2013); A1;,
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