Month: June 2021

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 4728-12-5, name is (2,2-Dimethyl-1,3-dioxan-5-yl)methanol. This compound has unique chemical properties. The synthetic route is as follows. Recommanded Product: 4728-12-5

To a solution of (2,2-dimethyl-l,3-dioxan-5-yl)methanol (1.078 g) in dichloromethane (20 mL) were added TEA (2.056 mL) and para-toluenesulfonyl chloride (1.687 g). The reaction mixture was stirred at room temperature for 4 hours and concentrated. The concentrate was partitioned between water and ethyl acetate. The organic layer was washed with brine, dried over Na2SO4, filtered and concentrated. The cruconcentrate was purified by flash chromatography (Analogix SF25chi40g with 10percent ethyl acetate/hexanes). MS (ESI) m/z 301.1 (M+l)+, 318.2 (M+18)+.

With the rapid development of chemical substances, we look forward to future research findings about 4728-12-5.

Reference:
Patent; ABBOTT LABORATORIES; WO2009/129385; (2009); A1;,
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Application of 349-75-7, 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. 349-75-7, name is (3-(Trifluoromethyl)phenyl)methanol, molecular formula is C8H7F3O, 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.

13.1 Ethyl 5-trimethylsilyl-1-[[(3-trifluoromethyl)phenyl]methyl]-1H-indole-2-carboxylate 0.51 ml (3.749 mmol) of 3-(trifluoromethyl)phenylmethanol and 0.9 g (3.749 mmol) of (cyanomethylene)tributylphosphorane (CMBP) are added, at ambient temperature, to a solution of 0.49 g (1.87 mmol) of ethyl 5-trimethylsilyl-1H-indole-2-carboxylate, obtained according to the protocol described in stage 3.4, in 8 ml of dry toluene, maintained under an inert atmosphere. The reaction mixture is stirred at 110 C. for 15 hours and then concentrated to dryness. The reaction crude is subsequently purified by flash chromatography on a silica gel column, elution being carried out with a mixture of hexane and ethyl acetate, to give 0.73 g of the expected ethyl 5-trimethylsilyl-1-[[(3-trifluoromethyl)phenyl]methyl]-1H-indole-2-carboxylate. 1H NMR (DMSO D6), delta (ppm): 7.90 (s, 1H); 7.62-7.57 (m, 2H); 7.51-7.43 (m, 3H); 7.40 (s, 1H); 7.17 (d, 1H); 5.92 (s, 2H); 4.28 (q, 2H); 1.26 (t, 3H); 0.27 (s, 9H). LC-MS: 420 ([M+H]+, Rt=3.62).

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 349-75-7, (3-(Trifluoromethyl)phenyl)methanol.

Reference:
Patent; SANOFI-AVENTIS; US2011/9365; (2011); A1;,
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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. 13826-35-2, name is (3-Phenoxyphenyl)methanol, molecular formula is C13H12O2, 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. Formula: C13H12O2

first step: A solution of IV-1 (3-phenoxyphenyl) methanol (0.5 g, 2.5 mmol) obtained in the previous step was dissolved in 30 ml of dichloromethane, and 20 ml of SOCl2 was added to 1 ml of DMF as a catalyst,25 C for 2 hours, After the TLC detection reaction was complete, the reaction solution was evaporated under reduced pressure to give excess SOCl2 to give a pale yellow oil IV-2 which was used directly in the next step.

With the rapid development of chemical substances, we look forward to future research findings about 13826-35-2.

Reference:
Patent; China Pharmaceutical University; Huang Wenlong; Qian Hai; Liu Chunxia; Li Zheng; Yang Jianyong; Bi Xinzhou; Cai Xingguang; (20 pag.)CN107162913; (2017); A;,
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Synthetic Route of 62285-58-9 , The common heterocyclic compound, 62285-58-9, name is (2,6-Dimethylphenyl)methanol, molecular formula is C9H12O, 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.

Step B: Preparation of Ethyl 2-(3-(2,6-dimethylbenzyloxy)-4-methoxyphenyl)acetate:; A solution of 2,6-Dimethylbenzyl alcohol (3.23 g, 23.7 mmol) and diisopropyl azodicarboxylate (DIAD, 5.23 g, 25.9 mmol) in THF (20 ml) was added drop wise to a solution of Ethyl 2-(3-Hydroxy-4-methoxyphenyl)acetate (Step A, 5.48 g, 26.12 mmol) and triphenylphosphine (6.79g, 25.9 mmol) in THF (100 ml) at O0C. The reaction mixture was stirred at room temperature for 4 hours, diluted with ether and washed with water and brine. The organic layer was dried over Na2SO4, filtered, concentrated, and purified by flash chromatography on a silica gel column (hex: ethyl acetate 4:1) to give the title compound. 1H NMR (270 MHz, CDCl3): 1.2 (t, 3H); 2.3 (s, 6H); 3.5 (s, 2H); 3.8 (s, 3H); 4.1 (q, 2H); 5.1 (s, 2H); 6.9 (m, 2H); 7.15-7.35 (m, 4H).

The synthetic route of 62285-58-9 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; WELLSTAT THERAPEUTICS CORPORATION; WO2009/151695; (2009); A1;,
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Adding a certain compound to certain chemical reactions, such as: 20017-67-8, 3,3-Diphenyl-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, 20017-67-8, blongs to alcohols-buliding-blocks compound. Product Details of 20017-67-8

Example 13 3-[4-(3,3-Diphenyl-propoxy)-phenyl]-2-ethoxy-propionic acid ethyl ester Reaction of 3,3-diphenyl-propan-1-ol (110 mg, 0.5 mmol), triphenylphosphine (145 mg, 0.55 mmol), 2-ethoxy-3-(4-hydroxy-phenyl)-propionic acid ethyl ester (140 mg, 0.6 mmol) and diethylazodicarboxylate (0.09 mL, 0.55 mmol) in an identical manner to Example 1 gave the title compound (120 mg). 1H NMR (CDCl3, 300 MHz); delta 1.10-1.29 (6H, 2*CH3), 2.44-2.55 (2H, CH2), 2.90-2.95 (2H, CH2), 3.28-3.39 and 3.51-3.62 (2H, OCH2), 3.80-3.89 (2H, CH2), 3.90-3.95 (1H, CHCO2), 4.10-4.28 (3H, arylCH and OCH2), 6.70-6.77 (2H, aryl), 7.05-7.35 (remaining H, aryl). MS calcd for C28H32O4 432.6, Found 432.3.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,20017-67-8, its application will become more common.

Reference:
Patent; Novo Nordisk, A/S; US6972294; (2005); B1;,
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Adding a certain compound to certain chemical reactions, such as: 80466-51-9, 1-(Benzylamino)-2-methylpropan-2-ol, 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, Product Details of 80466-51-9, blongs to alcohols-buliding-blocks compound. Product Details of 80466-51-9

A mixture of methyl 3-bromo-2-(bromomethyl)propanoate (1.2 equiv.), 1-(benzylamino)- 2-methylpropan-2-ol (1 equiv.), and potassium carbonate is dissolved in acetone. The solution is heated to reflux and allowed to stir until the starting material is consumed as judged by TLC or LCMS analysis. The mixture is then cooled to room temperature and filtered. The filtrate is evaporated under reduced pressure to give the desired cyclized adduct see for example PCT Int. Appl., 2010139481.

The synthetic route of 80466-51-9 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; C4 THERAPEUTICS, INC.; PHILLIPS, Andrew, J.; NASVESCHUK, Chris, G.; HENDERSON, James, A.; LIANG, Yanke; LAZARSKI, Kiel; MICHAEL, Ryan, E.; (771 pag.)WO2017/197036; (2017); A1;,
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In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 35364-79-5, name is 2-(3,4-Dichlorophenyl)ethanol, the common compound, a new synthetic route is introduced below. Computed Properties of C8H8Cl2O

General procedure: The starting material, 2-(3,4-dimethoxyphenyl)-ethan-1-ol (521 mg, 2.86 mmol, 1.0 equiv) was dissolved in dichloromethane (20 mL) and imidazole (583 mg, 8.58 mmol, 3.0 equiv) was added. The mixture was stirred for 5 minutes. tert-Butyldimethylsilyl chloride (518 mg, 3.43 mmol, 1.2 equiv) was added and the reaction mixture was stirred at room temperature for 1 hr. Water (20 mL) and dichloromethane (20 mL) were added and the mixture was shaken in a separating funnel. The aqueous layer was separated and washed with dichloromethane (2 x 5 mL). The combined organic layers were washed with water (20 mL), brine (20 mL) and dried over MgSO4. Following filtration, the solvent was removed under reduced pressure. The crude material was purified by column chromatography on silica gel (eluting with a gradient from petroleum ether to 1:1 petroleum ether : ether) to afford 820mg of 1a (97%).

The synthetic route of 35364-79-5 has been constantly updated, and we look forward to future research findings.

Reference:
Article; O’Brien, Matthew; Konings, Lisette; Martin, Matthew; Heap, Jordan; Tetrahedron Letters; vol. 58; 25; (2017); p. 2409 – 2413;,
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Reference of 23377-40-4, 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. 23377-40-4, name is 3-(Hexadecyloxy)propan-1-ol, molecular formula is C19H40O2, 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.

To a mixture of adefovir (1.36 g, 5 mmol) and 3-hexadecyloxy-l-propanol (1.8 g, 6 nunol) in dry pyridine was added DCC (2.06 g, 10 mmol). The mixture was heated to reflux and stirred 18 h then cooled and filtered. The filtrate was concentrated under reduced pressure and the residue was applied to a short column of silica gel. Elution of the column with 9:1 dichloromethane/methanol yielded hexadecyloxypropyl-adefovir (HDP-ADV) as a white powder.

According to the analysis of related databases, 23377-40-4, the application of this compound in the production field has become more and more popular.

Reference:
Patent; CHIMERIX, INC.; WO2006/110656; (2006); A2;,
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Application of 4152-92-5, 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. 4152-92-5, name is (2-(Aminomethyl)phenyl)methanol, molecular formula is C8H11NO, 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 1(3R,6f?)-3-(2,3-Dihydro-1 H-inden-2-yl)-6-(1 -ethylpropyl)-1 -[2(hydroxymethyl)- benzyI]piperazine-2,5-dione [2-(Aminomethyl)phenyl]methanol (4.12g, 30 mmol) was dissolved in methanol (30ml) and 2-ethylbutanal (3.7ml, 30 mmol) added followed by (2R)-2,3-dihydro-1H-inden-2- yl({[(1 ,1-dimethylethyl)oxy]carbonyl}amino)ethanoic acid (8.74g, 30 mmol). The mixture was stirred for 15 minutes before 4-chlorophenylisonitrile (4.13g, 30 mmol) was added. The mixture was stirred for 2.25 hours and then left to stand at room temperature overnight (16.3 hours) before it was cooled in an ice / water bath. Then acetyl chloride (12.75ml, 179.5 mmol) was added dropwise, keeping the reaction temperature below 200C. Then the mixture was stirred in the cooling bath for a further 10 minutes before it was stirred at room temperature. After 5 hours the mixture was evaporated under reduced pressure to leave a dark brown gum. The gum was stirred in chloroform (75ml) and saturated aqueous sodium bicarbonate solution (75ml) for 20 minutes before it was diluted with chloroform (75ml) and the phases separated. The aqueous phase was extracted with chloroform (3 * 75ml). The combined organic phase was dried (MgSO4) and concentrated under reduced pressure to ca. 75ml. The chloroform solution was treated with glacial acetic acid (3ml) and left to stand, at room temperature over the weekend. Then the reaction mixture was washed with 2M hydrochloric acid (75ml), followed by saturated aqueous sodium bicarbonate solution (75ml). The organic phase was dried (MgSO4) and evaporated under reduced pressure and dried to leave a brown foam. The foam was loaded in dichloromethane onto a 33Og flash silica chromatography column (pre-eluted with 20% ethyl acetate in cyclohexane). The column was eluted with 20% to 100% ethyl acetate in cyclohexane to afford (3f?,6R)-3-(2,3-dihydro-1H-inden-2- yl)-6-(1-ethylpropyl)-1-[2-(hydroxymethyl)benzyl]piperazine-2,5-dione (4.12g) as a pale brown solid. HPLC (A) Rt = 3.26 minutes; m/z [M+H]+ = 421. EPO 1H NMR (CDCI3) delta 7.37 (m, 1 H), 7.30 (m, 2H), 7.21 (m, 5H), 6.84 (br d,1 H), 5.45 (d, 1 H), 4.74 and 4.63 (d, 2H), 4.16 (d, 1 H), 4.08 (dd, 1 H), 4.04 (d, 1 H), 3.15 (m, 3H), 2.92 (m, 1H), 2.78 (m, 2H), 1.76 (m, 1 H), 1.62 (m, 3H), 1.31 (m, 1 H), 0.92 (m, 6H).

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 4152-92-5, (2-(Aminomethyl)phenyl)methanol.

Reference:
Patent; GLAXO GROUP LIMITED; WO2006/67462; (2006); A1;,
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Application of 5456-63-3, 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.5456-63-3, name is trans-2-Aminocyclohexanol hydrochloride, molecular formula is C6H14ClNO, molecular weight is 151.6345, as common compound, the synthetic route is as follows.

To a suspension of l-(2,4-dichlorophenyl)-4-hydroxymethyl-5-[4-(3,3,3-trifluoropropane- l-sulfonyloxy)phenyl]-lH-pyrazole-3-carboxylic acid (0.70 g, 1.30 mmol) in dichloromethane (90 ml) was added c-2-aminocyclohexanol hydrochloride (200 mg, 1.32 mmol) followed by triethylamine (0.37 ml, 2.63 mmol) and BOP (708 mg, 1.60 mmol). The reaction mixture was stirred at room temperature overnight, poured into ice- water and extracted with EtOAc (x3). The combined organic extracts were dried (Na2SO4), filtered and concentrated. Flash chromatography (heptane : EtOAc 50 : 50 – EtOAc) and CH2Cl2 : MeOH 99 : 1 – 95 : 5) afforded 200 mg (24%) of the title compound as a colorless solid. HPLC: 89%. MS: 658 (M+Na).

The chemical industry reduces the impact on the environment during synthesis 5456-63-3, I believe this compound will play a more active role in future production and life.

Reference:
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2007/148061; (2007); A1;; ; Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2007/148062; (2007); A1;,
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