Month: March 2021

Related Products of 6850-39-1, 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.6850-39-1, name is 3-Aminocyclohexanol, molecular formula is C6H13NO, molecular weight is 115.17, as common compound, the synthetic route is as follows.

To a solution of 5-chloro-3-(5-fluoro-4-(methylsulfonyl)pyrimidin-2-yl)-1-tosyl-1H-pyrrolo[2,3-b]pyridine, 1a, (1.09 g, 2.34 mmol) and 3-aminocyclohexanol (0.32 g, 2.82 mmol) in THE was added DIEA (0.60 g, 4.69 mmol). The reaction mixture was heated at 130 C. in microwave for 10 min. The solvent was removed under reduced pressure and the resulting residue was purified by silica gel chromatography to afford 550 mg of the desired product, 27a.

The chemical industry reduces the impact on the environment during synthesis 6850-39-1, I believe this compound will play a more active role in future production and life.

Reference:
Patent; VERTEX PHARMACEUTICALS INCORPORATED; CHARIFSON, PAUL S; CLARK, MICHAEL P; BANDARAGE, UPUL K; BETHIEL, RANDY S; COURT, JOHN J; DENG, HONGBO; DAVIES, IOANA; DUFFY, JOHN P; FARMER, LUC J; GAO, HUAI; GU, WENXIN; JACOBS, DYLAN H; KENNEDY, JOSEPH M; LEDEBOER, MARK W; LEDFORD, BRIAN; MALTAIS, FRANCOIS; PEROLA, EMANUELE; WANG, TIAN-SHENG; WANNAMAKER, M WOODS; BYRN, RANDAL; CHOU, II; LIN, CHAO; JIANG, MIN; JONES, STEVEN; GERMANN, URSULA A; SALITURO, FRANCESCO G; KWONG, ANN DAK-YEE; (541 pag.)JP2015/38146; (2015); A;,
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Related Products of 395-23-3, The major producers of chemicals have been the Europe, Japan and China. Due to the growing call for a cleaner, greener environment, people will have to find innovative ways to maintain their relevance. Here is a compound 395-23-3, name is Phenyl(4-(trifluoromethyl)phenyl)methanol. This compound has unique chemical properties. The synthetic route is as follows.

General procedure: To a solution of substrate 2a2t(0.100 mmol), Cs2CO3 (24.4 mg, 75.0mol) and catalyst1d(4.8 mg, 5.00mol) inEt2O (3.00 mL)was added isobutyric anhydride (12.4L, 75.0mol)at60 C. The reaction mixture was stirred for 15 h at60 C.MeOH (2 mL) was then added to destroy unreactedisobutyricanhydride and the mixture was stirredfor 30 minasit warmedto room temperature. The resulting solution was concentratedin vacuo. The resulting mixture was passed through a short padofsilica gel(eluent: hexane/Et2O=1/1, v/v) to give the esterproduct and the unreacted alcohol,which were directly analyzed by chiralHPLC. The enantiomeric ratio (er) and enantiomeric excess (ee) values ofthe ester and the unreacted alcoholwere obtained by HPLC analysis. The conversion (C) and sfactor (s)ofkinetic resolution were calculated asfollows:52sln1C1ee0ln1C1ee0ln1C1eeln1C1eekfastkslow2eeenantiomeric excess measuredfor the starting material3ee0enantiomeric excess measuredfor the product 4Ceeeeee0100conversion 5

According to the analysis of related databases, 395-23-3, the application of this compound in the production field has become more and more popular.

Reference:
Article; Fujii, Kazuki; Mitsudo, Koichi; Mandai, Hiroki; Suga, Seiji; Bulletin of the Chemical Society of Japan; vol. 89; 9; (2016); p. 1081 – 1092;,
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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. 756520-66-8, name is 1-(2,6-Dichloro-3-fluorophenyl)ethanol. A new synthetic method of this compound is introduced below., Recommanded Product: 756520-66-8

To a solution of 1-(2,6-dichloro-3-fluorophenyl)ethan-1-ol 18 (19.00 g, 90.89 mmol) in 150 ml of CH2Cl2 was added Et3N (13.27 ml, 95.43 mmol) and catalytic amount of DMAP. The resulting solution was cooled in an ice bath and added dropwise MsCl (7.39 ml, 95.43 mmol). After complete addition of MsCl, the reaction mixture was maintained in the ice bath for 1 h and then 30 ml of water was added to the reaction mixture. The organic phase was washed with brine, dried over anhydrous Na2SO4 and concentrated under vacuum. The crude product was pure enough for use in the next step. 1H NMR (300 MHz, CDCl3) delta 7.33 (dd, J = 4.8, 9.0 Hz, 1H), 7.12 (dd, J = 8.1, 9.0 Hz, 1H), 6.45 (q, J = 6.9 Hz, 1H), 2.91 (s, 3H), 1.84 (d, J = 6.9 Hz, 3H).

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, 756520-66-8, 1-(2,6-Dichloro-3-fluorophenyl)ethanol.

Reference:
Article; Zhang, Dengyou; Ai, Jing; Liang, Zhongjie; Li, Chunpu; Peng, Xia; Ji, Yinchun; Jiang, Hualiang; Geng, Meiyu; Luo, Cheng; Liu, Hong; Bioorganic and Medicinal Chemistry; vol. 20; 17; (2012); p. 5169 – 5180;,
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Application of 4740-78-7, 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. 4740-78-7, name is 1,3-Dioxan-5-ol, molecular formula is C4H8O3, 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.

Example 14 and Example 15; In 2 ml of tetrahydrofuran were dissolved 224 mg of the compound represented by the formula (IIa-1) and 125 mg of glycerol formal, 50 mg of sodium hydride was added under ice-cooling, and the mixture was stirred at room temperature for 2 hours. Thereafter, an aqueous saturated ammonium chloride was added to the reaction mixture, followed by extraction with t-butyl methyl ether. The organic layer was dried with sodium sulfate, and concentrated under reduced pressure. The residue was subjected to medium pressure preparative liquid chromatography to obtain 67 mg of a compound represented by the formula (14) :(hereinafter, referred to as present compound (14)) and 74 mg of a compound represented by the formula (15) :(hereinafter, referred to as present compound (15) . Present compound (14)1H-NMR (CDCl3, TMS) delta (ppm) : 5.07 (IH, s) , 4.93 (IH, s), 4.59 (2H, m) , 4.47 (IH, m) , 4.04 (IH, dd) , 3.79 (IH, dd) , ‘3.04 (6H, br)Present compound (15)1H-NMR (CDCl3, TMS) delta (ppm): 5.06 (IH, m) , 5.03 (IH, d) , 4.83 (IH, d) , 4.26 (2H, dd) , 4.08 (2H, dd) , 3.04 (6H, br)

While traditionally a conservative industry, chemical producers will need to modernize their PR strategies to stay relevant.we look forward to future research findings about 4740-78-7, 1,3-Dioxan-5-ol.

Reference:
Patent; SUMITOMO CHEMICAL COMPANY, LIMITED; WO2008/32858; (2008); A2;,
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Synthetic Route of 17100-58-2, Adding some certain compound to certain chemical reactions, such as: 17100-58-2, name is (4-Bromo-2-methylphenyl)methanol,molecular formula is C8H9BrO, 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 17100-58-2.

Scheme 1, step B: Methanesulfonyl chloride (171 mL, 2.11 mol) is added over 30 minutes to a mixture of (4-bromo-2-methyl-phenyl)methanol (250 g, 1.24 mol) and triethylamine (304 mL; 2.11 mol) in dichloromethane (2500 mL) cooled in ice/water. The mixture is allowed to warm to ambient temperature and is stirred for 16 hours. Water (5000 mL) is added and the product is extracted with dichloromethane (2*7000 mL). The combined organic layers are washed with saturated aqueous NaCl solution (5000 mL) and dried over Na2SO4 Filtration and concentration under reduced pressure provides a residue which is passed through a silica pad (eluting with hexane and ethyl acetate) to provide the title compound (234 g; 86% yield).

According to the analysis of related databases, 17100-58-2, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Eli Lilly and Company; QU, Fucheng; US2014/100179; (2014); A1;,
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Synthetic Route of 40571-86-6, 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.40571-86-6, name is Trans-2-(benzylamino)cyclohexanol, molecular formula is C13H19NO, molecular weight is 205.2961, as common compound, the synthetic route is as follows.

B. (S)-Mandelic acid salt of (1R,2R)-2-trans-2-(benzylamino)cyclohexanol (3) and (R)-Mandelic acid salt of (1S,2S)-2-trans-2-(benzylamino)cyclohexanol (ent-3): A 1-L single-necked, roundbottomedflask containing equipped with a mechanical stirrer and apressure-equalising addition funnel was charged with the preparedethyl acetate solution (300 mL) containing amino alcohol rac-2, and asolution of (S)-mandelic acid (70.4 g, 0.46 mol, 0.5 equiv.) in EtOAc(150 mL) was added via the addition funnel over a period of 2 h atroom temperature. After the addition was complete the droppingfunnel was rinsed with EtOAc (2 ¡Á 5 mL) and the reaction mixture wasstirred overnight at ambient temperature, followed by 5 h at 0 C. Theprecipitated ammonium salt was collected by suction filtration, washedwith ethyl acetate (2 ¡Á 50 mL), and dried under reduced pressure at roomtemperature over 1 h to afford the (S)-mandelic acid salt of (1R,2R)-2-trans-2-(benzylamino)cyclohexanol (3) as a colourless solid (131.8 g,0.37 mol), yield 80% based on mandelic acid, m.p. 147-149 C (lit.10146 C); [alpha]D25 = +14.7 (c = 2.0, CHCl3); 1H NMR (CDCl3) delta 0.96-1.29(m, 4 H), 1.58-1.73 (m, 3 H), 1.90 (d, J = 12.6 Hz, 1 H), 2.53 (dt, J = 4.0,J = 12.0 Hz, 1 H), 3.03 (dt, J = 4.3, 10.6 Hz, 1 H), 3.46 (d, J = 12.9 Hz, 1H), 3.89 (d, J = 12.6 Hz, 1 H), 4.90 (s, 1 H), 7.19-7.35 (m, 8 H), 7.49-7.52(m, 2H). The filtrate from the above procedure was concentrated underreduced pressure to give a pale yellow oily residue (518.2 g) which wasdissolved in EtOAc (200 mL), transferred into a 1-L flask, and treatedwith a solution of (R)-mandelic acid ((70.4 g, 0.46 mol, 0.5 equiv.) inethyl acetate (100 mL) similar to the above described procedure, todeliver the (R)-mandelic acid salt of (1S,2S)-2-trans-2-(benzylamino)cyclohexanol (ent-3) as a colourless solid (132.8 g, 0.36 mol), yield 78%based on mandelic acid), [alpha]D25 = -15.3 (c = 2.0, CHCl3). The analyticaldata were in accordance with those observed for the correspondingenantiomer of opposite configuration.

The chemical industry reduces the impact on the environment during synthesis 40571-86-6, I believe this compound will play a more active role in future production and life.

Reference:
Article; Xue, Feng; Li, Chang-Gong; Zhu, Yong; Lou, Tian-Jun; Journal of Chemical Research; vol. 38; 5; (2014); p. 322 – 324;,
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Application of 5259-98-3, 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. 5259-98-3, name is 5-Chloropentan-1-ol, molecular formula is C5H11ClO, 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.

Under a nitrogen atmosphere, 5.0 g of the compound represented by the formula (I-8-12), 0.2 g of pyridinium p-toluenesulfonate and 30 mL of dichloromethane were added to the reaction vessel. 3.8 g of 3,4-dihydro-2H-pyran was added with ice cooling and the mixture was stirred. After washing with a saturated aqueous solution of sodium bicarbonate and brine, purification was carried out by column chromatography (alumina, dichloromethane) to obtain 7.6 g of the compound represented by the formula (I-8-13).

According to the analysis of related databases, 5259-98-3, the application of this compound in the production field has become more and more popular.

Reference:
Patent; DIC CORPORATION; HORIGUCHI, MASAHIRO; AOKI, YOSHIO; HAYASHI, TAKUO; TSURUTA, TORU; (69 pag.)JP2017/218391; (2017); A;,
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Reference of 96-35-5, 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 96-35-5 as follows.

To a suspension of KOtBu (996.6 mg, 8.881 mmol) in THF (640.4 mg, 8.881 mmol) cooled to 0 C was added dropwise methyl 2-hydroxyacetate (675.7 mu, 8.881 mmol) and stirred for 10 minutes. The acrylonitrile (589.1 mu, 8.881 mmol) was then added and the reaction stirred at ambient temperature. After 3 hours, the reaction was diluted with H20 (50 mL), then extracted with Et20 (25 mL) to remove any starting ester. The basic aqueous phase was acidified with 2M HCl (5 mL), then extracted with Et20 (2 x 50 mL). The combined organic phases were dried with MgS04, filtered, and concentrated to afford a light brown oil (446 mg, 45.2% yield). FontWeight=”Bold” FontSize=”10″ H NMR (CDC13) delta 4.63 (t, 1H), 4.24 (t, 1H), 4.14 (d, 1H), 4.02 (d, 1H), 3.57 (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,96-35-5, its application will become more common.

Reference:
Patent; ARRAY BIOPHARMA INC.; ALLEN, Shelley; ANDREWS, Steven, Wade; BLAKE, James, F.; BRANDHUBER, Barbara, J.; HAAS, Julia; JIANG, Yutong; KERCHER, Timothy; KOLAKOWSKI, Gabrielle, R.; THOMAS, Allen, A.; WINSKI, Shannon, L.; WO2014/78454; (2014); A1;,
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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. 3279-95-6, name is 2-(Aminooxy)ethanol. A new synthetic method of this compound is introduced below., Recommanded Product: 3279-95-6

General procedure: 4a-c (1 equiv) were dissolved in ethanol (10mL). O-(2-hydroxyethyl)hydroxylamine (14, 2 equiv), acetic acid (2 equiv), pyridine (2 equiv) were added to the solution. After being refluxed for 5h, ethanol was removed under reduced pressure. The products were extracted with CH2Cl2. The combined extracts were washed with 2M HCl aqueous solution and brine. The organic layer was dried with anhydrous Na2SO4. The solvent was removed under reduced pressure and the residue was purified by column chromatography (PE: EtOAc=6: 1) to yield 15a-c.

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, 3279-95-6, 2-(Aminooxy)ethanol.

Reference:
Article; Li, Haihong; Wang, Ke; Wan, Qi; Chen, Ying; Steroids; vol. 141; (2019); p. 81 – 95;,
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Related Products of 124-68-5, 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. 124-68-5, name is 2-Amino-2-methyl-1-propanol. A new synthetic method of this compound is introduced below.

(3a) (2-Hydroxy-1,1-dimethylethyl)carbamic acid t-butyl ester 230.4 ml of di-t-butyl dicarbonate (1.00 mol) was added to a solution of 98.05 g of 2-amino-2-methyl-1-propanol (1.10 mol) and 154 ml of triethylamine (1.10 mol) in methylene chloride (500 ml) at room temperature over 20 minutes, and the mixture was stirred at room temperature for 2.5 hours. The reaction mixture was concentrated under reduced pressure and diluted with a 10% citric acid aqueous solution, followed by extraction with ethyl acetate. Then, the organic layer was washed with water and brine and dried over anhydrous magnesium sulfate. After filtration, the solvent was evaporated under reduced pressure to obtain 189.25 g of the crude title compound (yield: quant.). Colorless solid. 1H NMR spectrum (CDCl3, 400 MHz), delta: 4.64 (br s, 1H), 4.01 (br s, 1H), 3.59 (d, 2H, J = 6.3 Hz), 1.43 (s, 9H), 1.25 (s, 6H).

At the same time, in my other blogs, there are other synthetic methods of this type of compound,124-68-5, 2-Amino-2-methyl-1-propanol, and friends who are interested can also refer to it.

Reference:
Patent; Daiichi Sankyo Company, Limited; EP2036896; (2009); A1;,
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