Month: November 2020

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.3973-18-0, name is Propynol ethoxylate, molecular formula is C5H8O2, molecular weight is 100.1158, as common compound, the synthetic route is as follows.3973-18-0

General procedure: To a 0.30mL of a solution of azide 14 (23mM in tBuOH-H2O (2: 1)) in an eppendorf, 0.10mL of a solution of the corresponding alkyne (a-s) (83mM in tBuOH) was added followed by 25muL of an aqueous solution of sodium ascorbate (30mM) and 25muL of an aqueous solution of CuSO4 (9.4mM). The final concentration of the azide 14 in each eppendorf was 15mM. The resulting mixtures were shaken at room temperature for 24h and monitored for completion by TLC and ESI-MS (see Supplementary data for mass spectra analysis). Then, the reactions were diluted with water to the desired concentration and placed in a 96-well microtiter plate in order to perform the enzymatic assays. In the preliminary screening of the resulting crude (pyrrolidin-2-yl)triazoles 14a-s, % of inhibition towards beta-glucosidase from almonds was determined at 10muM of the pyrrolidine-triazole on each well (assuming quantitative conversion in the click reaction).

Statistics shows that 3973-18-0 is playing an increasingly important role. we look forward to future research findings about Propynol ethoxylate.

Reference:
Article; Martinez-Bailen, Macarena; Carmona, Ana T.; Moreno-Clavijo, Elena; Robina, Inmaculada; Ide, Daisuke; Kato, Atsushi; Moreno-Vargas, Antonio J.; European Journal of Medicinal Chemistry; vol. 138; (2017); p. 532 – 542;,
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456-47-3, 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. 456-47-3, name is 3-Fluorobenzyl alcohol, molecular formula is C7H7FO, 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.

General procedure: A 20-mL test-tube equipped with a magnetic stirring bar was charged with o-nitroaniline 1 (2.5 mmol, 1 equiv), alcohol 2 or 5 (3 mmol, 1.2equiv), Na2S¡¤nH2O (?60%, 130 mg, 1 mmol, 40 mol%) and FeCl3¡¤6H2O(7 mg, 0.025 mmol, 1 mol%). The resulting mixture was stirred for 24h under an argon atmosphere at the indicated temperature (see Schemes 2 and 3 and Table 2). After cooling to r.t., the mixture was purified in different ways. (i) For NH benzimidazole products, the mixture was washed with CH2Cl2 (3 ¡Á 2 mL) then dissolved in MeOH.The MeOH solution was filtered through a short pad of silica gel. The filtrate was concentrated in vacuo to afford the NH benzimidazole product. Further purification by column or recrystallization was carried out if necessary. (ii) For N-methyl-2-phenylbenzimidazole 3ha and quinoxalines 5, the crude mixture was dissolved in a minimum volume of CH2Cl2 and purified by column chromatography (silica gel or alumina, heptane-EtOAc, EtOAc, EtOAc-MeOH, hexane-Et2O). We noted that some 13C NMR signals of NH-benzimidazoles are missing or difficult to observe.

In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles. 456-47-3, 3-Fluorobenzyl alcohol, other downstream synthetic routes, hurry up and to see.

Reference:
Article; Nguyen, Thanh Binh; Ermolenko, Ludmila; Al-Mourabit, Ali; Synthesis; vol. 47; 12; (2015); p. 1741 – 1748;,
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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.39590-81-3, name is 1,1-Bis(Hydroxymethyl)cyclopropane, molecular formula is C5H10O2, molecular weight is 102.13, as common compound, the synthetic route is as follows.39590-81-3

5 g of cyclopropane-1,1-diyldimethanol are solubilized in 31 mL of pyridine. Cooling is performed down to 0-5 C., and then 10.3 mL of mesyl chloride are added dropwise, stirring is performed for 2 h. Add 40.46 mL of H2O+12.24 mL of concentrated HCl in order to precipitate the compound. The precipitate is filtered and dried in the oven. 10 g (yield=80%) of cyclopropane-1,1-diylbis(methylene)dimethanesulfonate are obtained as a white powder:

Statistics shows that 39590-81-3 is playing an increasingly important role. we look forward to future research findings about 1,1-Bis(Hydroxymethyl)cyclopropane.

Reference:
Patent; SANOFI; Arigon, Jerome; Brollo, Maurice; Clement, Jacques; Combet, Romain; Durand, Florence; El Ahmad, Youssef; Labrosse, Jean-Robert; Letallec, Jean-Philippe; Ronan, Baptiste; US2013/289031; (2013); A1;,
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702-82-9, 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. 702-82-9, name is 3-Aminoadamantan-1-ol, molecular formula is C10H17NO, 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.

General procedure: A mixture of 0.136 or 0.272 g (1 or 2 mmol) of 1-oxa-3,6-dithiacycloheptane (1) [3] in 5 mL of chloroform and 0.018 g (0.05 mmol) of SmCl3 ¡¤ 6 H2O was stirred for 30 min at room temperature under argon, and a solution of 1 mmol of the corresponding amine in 5 mL of ethanol was added dropwise. The mixture was stirred for 3 h at room temperature, treated with 2 mL of water, stirred for 30 min more, and extracted with chloroform (20 mL). The extract was evaporated, and the product (compound 2-17) was isolated from the residue by column chromatography on silica gel.

In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles. 702-82-9, 3-Aminoadamantan-1-ol, other downstream synthetic routes, hurry up and to see.

Reference:
Article; Rakhimova; Ismagilov; Khalilov; Zainullin; Ibragimov; Dzhemilev; Russian Journal of Organic Chemistry; vol. 51; 7; (2015); p. 951 – 956; Zh. Org. Khim.; vol. 51; 7; (2015); p. 971 – 976,6;,
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Adding some certain compound to certain chemical reactions, such as: 56239-26-0, name is cis-4-Aminocyclohexanol hydrochloride, 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 56239-26-0. 56239-26-0

Cis-4-Aminocyclohexanol hydrochloride (Aldrich cat740365: 8.3 mg, 0.055 mmol) was added to a solution of 5-(3-phenylpiperidin-1-yl)pyridine-2-carbaldehyde (10 mg, 0.04 mmol) in N,N-dimethylformamide, followed by acetic acid (0.11 mmol). After 5 min, sodium cyanoborohydride (6.9 mg, 0.11 mmol) was added. The reaction mixture was stirred at room temperature overnight. The crude reaction mixture was purified by prep LCMS (pH 2, acetonitrile/water+TFA) to give the desired product as its TFA salt. LC-MS calculated for C23H32N3O (M+H)+: m/z 366.3; found: 366.3.

Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of 56239-26-0.

Reference:
Patent; Incyte Corporation; Wu, Liangxing; Qian, Ding-Quan; Lu, Liang; Lajkiewicz, Neil; Konkol, Leah C.; Li, Zhenwu; Zhang, Fenglei; Li, Jingwei; Wang, Haisheng; Xu, Meizhong; Xiao, Kaijiong; Yao, Wenqing; (101 pag.)US2018/177784; (2018); A1;,
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156-87-6, A common compound: 156-87-6, name is 3-Aminopropan-1-ol,molecular formula is C3H9NO, it can change the direction of chemical reaction, and react with certain compounds to generate new functional products. A new synthetic method of this compound is introduced below.

To a stirred mixture of 3-aminopropan-1-ol (10.00 mmol, 751 mg) and benzaldehyde (10 mmol, 1061 mg) in dichloromethane (35 ml) was added sodium triacetoxyborohydride (14.00 mmol, 2967 mg). The reaction was stirred overnight then quenched with methanol (200ml) and product isolated by SCX (eluting with 7N ammonia in MeOH). Evaporation gave 0.85 g of 3-(benzylamino)propan-1-ol (51 % yield), EI-MS: m/z = 166.4 [M+H]+.

With the rapid development of chemical substances, we look forward to future research findings about 156-87-6.

Reference:
Patent; N.V. ORGANON; WO2009/37220; (2009); A1;,
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Adding some certain compound to certain chemical reactions, such as: 1074-16-4, name is 2-(2-Bromophenyl)ethanol, 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 1074-16-4. 1074-16-4

Step 3: 2-(2-bromophenyl)acetaldehydeTo a suspension of PCC (5.9 g, 28 mmol) in DCM (15 mL) was added a solution of 2- (2-bromophenyl)ethanol (3.7 g , 18 mmol) in DCM (20ml_) at room temperature whereupon a slightly exothermic reaction took place with the formation of a black reaction mixture which was kept stirring at room temperature for 15 hours. Then, ethyl ether (150 mL) was added and the mixture was filtered through silica gel on a pad of celite. The residue was washed with ether (50ml_) and the filtrate was concentrated under reduced pressure to afford crude product 2-(2-bromophenyl)acetaldehyde (3.4 g, 17 mmol, 94 % yield) as a light black oil. LCMS (m/z, ES 199 (M+H)

Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of 1074-16-4.

Reference:
Patent; GLAXO GROUP LIMITED; JOHNS, Brian Alvin; SHOTWELL, John Brad; HAIGH, David; WO2012/67663; (2012); A1;,
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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.623-04-1, name is (4-Aminophenyl)methanol, molecular formula is C7H9NO, molecular weight is 123.1525, as common compound, the synthetic route is as follows.623-04-1

To a solution of (4-Aminophenyl)methanol (1.50 g, 12.18 mmol) in CH2CI2 (20 ml.) was added TBDMSCI (1.84 g, 12.18 mmol) and imidazole (0.91 g, 13.40 mmol). After stirring for 1 h at room temperature, the solution was diluted with brine, and extracted with E-tOAc. The organic extract was dried (Na2SO4), filtered, and evaporated. The residue was purified by silica gel column chromatography with gradient of EtOAc (25-100%) in Hexane to afford 67 (2.76 g, 96%) as a light yellow oil. LRMS (ESI): (calc.) 237.4; (found) 238.2 (MH) +

Statistics shows that 623-04-1 is playing an increasingly important role. we look forward to future research findings about (4-Aminophenyl)methanol.

Reference:
Patent; METHYLGENE INC.; WO2006/102760; (2006); A1;,
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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 25646-77-9, name is 2-((4-Amino-3-methylphenyl)(ethyl)amino)ethanol sulfate. This compound has unique chemical properties. The synthetic route is as follows. 25646-77-9

To a solution of 4.39 g (0.015 mol) of 2-[(4-amino-3- methylphenyl)(ethyl)amino]ethanol sulfate in 5 ml of water and 10 ml of ethanol is added a solution of 4-butoxybenzene- 1 ,3-diamine dihydrochloride in 5 ml of water and 10 ml of ethanol. The pH is adjusted to 9.5 with 15 ml of 20% aqueous ammonia. 51 ml of 6% aqueous hydrogen peroxide solution are added and the mixture is stirred for 12 hours. The resulting mixture is extracted with butanol. The organic phase is washed with water brought to pH 10.5 with 20%) aqueous ammonia. The organic phase is dried with disodium sulfate and filtered, and the butanol is then evaporated off. The product is washed with isopropyl ether and filtered off.2.81 g of 2- {[4-(2-amino-5-butoxy-4-iminocyclohexa-2,5-dienylideneamino)-3- methylphenyljethylamino} ethanol 2 are obtained in the form of a black product. The molecular ion 371 (ES+) is detected by mass spectrometry.

Statistics shows that 25646-77-9 is playing an increasingly important role. we look forward to future research findings about 2-((4-Amino-3-methylphenyl)(ethyl)amino)ethanol sulfate.

Reference:
Patent; L’OREAL; SABELLE, Stephane; LEDUC, Madeleine; WO2013/87636; (2013); A1;,
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575-03-1 , The common heterocyclic compound, 575-03-1, name is 7-Hydroxy-4-(trifluoromethyl)coumarin, molecular formula is C10H5F3O3, 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.

(1) to 10 ml containing 0.5mmol of 4 – trifluoromethyl -7 – hydroxy coumarin and 0.625mmol of triethylamine in tetrahydrofuran solution, slowly dropping 0.6mmol to the propyl benzoyl chloride (dissolved in 5 ml of in tetrahydrofuran), to control the temperature 0 ¡ãC;(2) stirring ice 1h after, solution to return to room temperature, stirring overnight;(3) the reaction solution through the pressure reducing and removing the solvent, the solid residue is purified by silica gel chromatography, using ethyl acetate-hexane – (1:3 v/v) elute, shall be 148 mg white solid powdery pure product.

According to the analysis of related databases, 575-03-1, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Da Lianli Technology Changshu Institute Co., Ltd.; Cui Jingnan; Feng Lei; (11 pag.)CN104592985; (2017); B;,
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