Day: July 21, 2021

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. 17874-79-2, name is 5-(Methoxycarbonyl)picolinic acid, the common compound, a new synthetic route is introduced below. Product Details of 17874-79-2

A solution of 5-(methoxycarbonyl)picolinic acid (3.33 g, 18.4 mmol) in a mixture of pyridine (20 mL) and N,N-dimethylformamide (35 mL) was treated with 1,1′-carbonyldiimidazole (3.28 g, 20.2 mmol) at 45 C. for 2 hours. After cooling, 2,3-diaminobenzamide (HCl salt) (4.12 g, 18.4 mmol) was added and the mixture stirred at room temperature overnight. The mixture was concentrated and the residue used in the next step without further purification.

The synthetic route of 17874-79-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; ABBOTT LABORATORIES; US2009/30016; (2009); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Adding a certain compound to certain chemical reactions, such as: 874302-76-8, 4-nitrophenyl 2-(pyridin-2-yldisulfanyl)ethyl carbonate, 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, Quality Control of 4-nitrophenyl 2-(pyridin-2-yldisulfanyl)ethyl carbonate, blongs to pyridine-derivatives compound. Quality Control of 4-nitrophenyl 2-(pyridin-2-yldisulfanyl)ethyl carbonate

To a solution of cabazitaxel (2.00 g, 2.40 mmol) and 2-(2- pyridinyldithio)ethanol p-nitrophenyl carbonate (915 mg, 2.60 mmol) in dichloromethane (48 mL) was added DMAP (439 mg, 3.60 mmol). The solution was stirred at room temperature overnight, then washed with 0.1N HCl (3 x 20 mL), brine (50 mL), and dried with sodium sulfate. The solvent was removed in vacuo, the the remaining residue purified by silica gel chromatography (2:1 petroleum ether:ethyl acetate) to give 4? (2.50 g, 2.38 mmol, 99% yield). LCMS m/z: 1049 (M + 1).

The synthetic route of 874302-76-8 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; TARVEDA THERAPEUTICS, INC.; BILODEAU, Mark T.; SIMCOX, Mary; WHITE, Brian H.; KADIYALA, Sudhakar; WOOSTER, Richard; (178 pag.)WO2017/180834; (2017); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Reference of 1061357-89-8, 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 1061357-89-8 as follows.

A mixture of 2-bromo-5-fluoro-4-iodopyridine (6.8 g, 22.5 mmol), ethylene glycol (Sigma-Aldrich, St. Louis, MO, USA) (6.0 mL, 108.0 mmol), and potassium t-butoxide (Sigma-Aldrich, St. Louis, MO, USA ) (2.5 g, 22.7 mmol) in N-methylpyrrolidinone (10 mL) and THF (20 mL) was heated in a 60 oC bath. After 40 min, the mixture was removed from the oil bath and allowed to stir at RT for 14 h. The mixture was concentrated under reduced pressure. Additional potassium t-butoxide (0.5 g) and ethylene glycol (1.0 mL) were added and the reaction heated in an 80 oC bath for another 3 h then cooled to RT. ethyl acetate (200 mL) and water (150 mL) were added and the phases mixed and separated. The organic phase was washed with brine (75 mL) then evaporated to dryness under reduced pressure. Purification of the residue using silica gel chromatography (0 – 50% ethyl acetate in DCM) gave 2-((6-bromo-4-iodopyridin-3-yl)oxy)ethanol (3.1 g, 9.0 mmol, 40% yield). MS (ESI +ve ion) m/z: [M+1] = 343.8 / 345.8. 1H NMR (400 MHz, chloroFORM-d) _ 7.89 (s, 1H), 7.88 (s, 1H), 4.22 (td, J = 4.55, 6.36 Hz, 2H), 3.99-4.07 (m, 2H).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,1061357-89-8, its application will become more common.

Reference:
Patent; AMGEN INC.; ALLEN, Jennifer R.; BOURBEAU, Matthew P.; BROWN, James A.; CHEN, Ning; FROHN, Michael J.; FU, Zice; LIU, Longbin; LIU, Qingyian; PETTUS, Liping H.; QIAN, Wenyuan; REEVES, Corey; SIEGMUND, Aaron C.; (362 pag.)WO2018/112094; (2018); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Electric Literature of 1073182-59-8 , The common heterocyclic compound, 1073182-59-8, name is Methyl 5-amino-2-chloroisonicotinate, molecular formula is C7H7ClN2O2, 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.

[00481] To a stirred solution of (5-amino-2-chloro-isonicotinic acid methyl ester (1.3 g, 7 mmol) in DCM (30 mL) was added Et3N (1.4 g, 14 mmol) and cyclopropanecarbonyl chloride (1.1 g, 10.5 mmol) at 0 C. The mixture was stirred at room temperature overnight. The mixture was evaporated in vacuum. The residue was diluted with water (50 mL). The aqueous phase was extracted with EA (80 mL x2). The extracts were washed with water, dried over anhydrous Na2S04 and filtered. The filtrate was evaporated in vacuum to residue, which was purified by silica gel chromatography (from PE to PE/EA = 10/1) to give (1.0 g, yield: 56 %) of 2-chloro-5-(cyclopropanecarbonyl-amino)-isonicotinic acid methyl ester as yellow solid. ‘H NMR (400MHZ, DMSO-i/6): delta = 10.56 (brs, 1H), 8.79 (s, 1H), 7.23 (s, 1H), 3.82 (s, 3H), 1.87- 1.80 (m, 3H), 0.94-0.83 (m, 4H).

The synthetic route of 1073182-59-8 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; HEDRICK Michael P.; HERSHBERGER Paul M.; MALONEY Patrick R.; PEDDIBHOTLA Satyamaheshwar; PINKERTON Anthony B.; WO2015/200534; A2; (2015);,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

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.624-28-2, name is 2,5-Dibromopyridine, molecular formula is C5H3Br2N, molecular weight is 236.892, as common compound, the synthetic route is as follows.Recommanded Product: 2,5-Dibromopyridine

The suspension of 11a (3.12g, 13.11mmol) in 15mL of morpholine was reacted under microwave condition for lOOmin at 12O0C. After the reaction was complete, 20OmL of ethyl acetate was added. The resulting solution was washed with 0.1N HCl (5OmL), water (10OmL), 0.1N NaOH (5OmL) and water (10OmL) subsequently. The resulting organic layer was dried over anhydrous Na2SCK and evaporated to provide lib (3.19g, 99.7%).

At the same time, in my other blogs, there are other synthetic methods of this type of compound,624-28-2, 2,5-Dibromopyridine, and friends who are interested can also refer to it.

Reference:
Patent; XCOVERY, INC.; WO2008/88881; (2008); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

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. 907545-47-5, name is 2-Chloro-5-nitroisonicotinic acid, molecular formula is C6H3ClN2O4, 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: C6H3ClN2O4

Synthesis of the compound 34 The compound 33 (3 g, 0.017 mol) was added into thionyl chloride (20 mL), two drops of DMF was added to the above mixture, and then refluxed for 2 h. The thionyl chloride was evaporated off, an acetone (20mL) was added and stirred in an ice bath, ammoniae gas was charged, and then the reaction was run for 1 h before completed. Acetone was evaporated off, 30 mL of water and 30 mL of ethyl acetate were added to the residue, and then extraction was performed. The ethyl acetate layer was washed with the saturated aqueous solution of table salt and evaporated to being dry. The resulted product was recrystallized in ethanol (95percent) to obtain 0.8 g of a white solid product with a yield of 23.5percent. The melting point is 193.4-193.7°C(ethanol).

With the rapid development of chemical substances, we look forward to future research findings about 907545-47-5.

Reference:
Patent; Beijing Yiling Bioengineering Co., Ltd.; EP2366691; (2011); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

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 760207-83-8, name is 3-Bromo-5-chloropicolinonitrile. This compound has unique chemical properties. The synthetic route is as follows. Recommanded Product: 760207-83-8

A microwave vial was charged with 3-bromo-5-chloropicolinonitrile (1.40 g, 6.44 mmol) and dichlorobis(triphenyl-phosphine)palladium (II) (0.54 g, 0.77 mmol). The vial was evacuated and backfilled with nitrogen and 1,4-dioxane (10 mL) was added, followed by tri-n-butyl(vinyl)tin (2.45 mL, 7.73 mmol). The reaction mixture was heated at 100 C. for 1 h. The reaction mixture was diluted with water and EtOAc. The solvent was removed under reduced pressure. The crude material was absorbed onto a plug of silica gel and purified by chromatography through a Redi-Sep pre-packed silica gel column (40 g), eluting with a gradient of 10% to 50% EtOAc in hexane, to provide 5-chloro-3-vinylpicolinonitrile (0.72 g, 4.37 mmol, 67.9% yield) as white solid. [0908] 1H NMR (400 MHz, CHLOROFORM-d) delta 8.54 (d, J=2.25 Hz, 1H), 7.97 (dd, J=0.44, 2.30 Hz, 1H), 7.05 (dd, J=11.20, 17.56 Hz, 1H), 6.05 (d, J=17.41 Hz, 1H), 5.76 (d, J=11.05 Hz, 1H).

With the rapid development of chemical substances, we look forward to future research findings about 760207-83-8.

Reference:
Patent; WHITE, Ryan; ALLEN, Jennifer R.; EPSTEIN, Oleg; HONG, Fang-Tsao; HUA, Zihao; HUMAN, Jason Brooks; LOPEZ, Patricia; OLIVIERI, Philip R.; ROMERO, Karina; SCHENKEL, Laurie; STELLWAGEN, John; TAMAYO, Nuria A.; ZHENG, Xiao Mei; US2014/213581; (2014); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Application of 70298-88-3, 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. 70298-88-3, name is 2,2-Dimehtyl-N-pyridin-3-yl-propionamide, molecular formula is C10H14N2O, 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.

nBuLi (2.5M in hexanes, 56.2 ml_, 140.5 mmol) was dropwise added to a solution of the title compound of Preparation 1a (10 g, 56.2 mmol) and N,N,N’,N’-tetramethylethylene- diamine (TMEDA) (20.9 ml_, 140.5 mmol) in diethyl ether (338 ml.) at -78 0C under argon and the resulting mixture was stirred at that temperature for 15 minutes and at -10 0C for 2 hours. Then, the reaction mixture was cooled down to -780C and 2-methoxybenzaldehyde (19.52 g, 140.5 mmol) in 34 ml_ of dry tetrahydrofuran was carefully added. After 15 minutes, the cooling bath was removed and the mixture stirred overnight at room temperature. Subsequently, water (100 mL) was added to the flask and it was extracted with ethyl acetate (3 x 200 mL), the organic solution was washed with brine, dried over sodium sulphate and the solvent removed under reduced pressure. The residue was purified by column chromatography on silica flash, using hexane/ethyl acetate (4:1 ) as eluents, to yield the title compound (11.1 g, 63%) as a solid.

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 70298-88-3, 2,2-Dimehtyl-N-pyridin-3-yl-propionamide.

Reference:
Patent; LABORATORIOS ALMIRALL, S.A.; WO2007/96072; (2007); A2;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

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. 55338-73-3, name is 5-Amino-2-pyridinecarbonitrile. This compound has unique chemical properties. The synthetic route is as follows. HPLC of Formula: C6H5N3

A 18 ml vial was loaded with a mixture of 30% H2O2 (1 ml), 3N NaOH (3 ml) and MeOH (2.5 ml). To this mixture 5-Amino-pyridine-2-carbonitrile (450 mg, 3.78 mmole) was added at room temperature. Reaction mixture was stirred at rt for 45 minutes, TLC showed the starting material to be consumed. The mixture was diluted with water and filtered; the solid was washed with water and dried to give 480 mg product, 92% yield.

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, 55338-73-3, 5-Amino-2-pyridinecarbonitrile.

Reference:
Patent; Nivalis Therapeutics, Inc.; Wasley, Jan; Rosenthal, Gary J.; Sun, Xicheng; Strong, Sarah; Qiu, Jian; US9138427; (2015); B2;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Application of 588729-99-1, 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 588729-99-1, name is 3-Amino-5-bromo-2-chloropyridine. This compound has unique chemical properties. The synthetic route is as follows.

Thionyl chloride (60.1 mL, 823 mmol) was added dropwise over 60 min to water (361 mL), cooled to 0 C, maintaining the temperature of the mixture 0-7 C. The solution was allowed to warm to 18 C over 17 h. copper(l) chloride (218 mg, 2.2 mmol) was added to the mixture, and the resultant yellow-green solution was cooled to -3 C using an acetone/ ice bath. 2) HCI (195 mL, 6.418 mol)(37% w/w) was added, with agitation, to 5-bromo-2-chloro-3- pyridineamine (25 g, 121 mmol), maintaining the temperature of the mixture below 30 C with ice cooling. The reaction mixture was cooled to -5 C using an ice/acetone bath and a solution of sodium nitrite (14.72 g, 213 mmol) in water (58 mL) was added dropwise over 45 min, maintaining the temperature of the reaction mixture between -5 to 0 C, the resultant slurry was cooled to -2 C and stirred for 10 min.3) The slurry from step (2) was cooled to -5 C and added to the solution obtained from step 1 ) over 30 min, maintaining the temperature of the reaction mixture between -3 to 0 C ( the slurry from step b was maintained at -5 C throughout the addition). As the reaction proceeded, a solid began to precipitate. When the addition was complete, the reaction mixture was agitated at 0 C for 75 min. The suspended solid was collected by vacuum filtration, washed with water, and dried under vacuum to give 5- bromo-2-chloro- 3-pyridinesulfonyl chloride. ES-LCMS: m/z 271 .94, 269.97 (M-1 ).

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 588729-99-1, 3-Amino-5-bromo-2-chloropyridine.

Reference:
Patent; GLAXOSMITHKLINE LLC; BANKA, Anna, Lindsey; BOTYANSZKI, Janos; DICKERSON, Scott, Howard; DUAN, Maosheng; LEIVERS, Martin, Robert; MCFADYEN, Robert, Blount; MOORE, Christopher, Brooks; REDMAN, Aniko, Maria; SHOTWELL, John, Bradford; TAI, Vincent, W.-F.; TALLANT, Matthew, David; XUE, Jianjun; WO2012/37108; (2012); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem