Category: 1458-18-0

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. 1458-18-0, name is Methyl 3-amino-5,6-dichloropyrazine-2-carboxylate, This compound has unique chemical properties. The synthetic route is as follows., 1458-18-0

To a stirred mixture of methyl 3-amino-5, 6-dichloropyrazine-2-carboxylate (50 mg, 0.225 nMol, 1 equiv) and DIEA (87.31 mg, 0.676 nMol, 3 equiv) in DMSO was added morpholine (39.24 mg, 0.450 nMol, 2 equiv) in portions at room temperature . The resulting mixture was stirred for overnight at room temperature . The reaction was quenched with Water at room temperature. The precipitated solids were collected by filtration and washed with water (1×100 mL) , dried under vacuum to afford methyl 3-amino-6-chloro-5- (morpholin-4-yl) pyrazine-2-carboxylate (1.8 g, 97.71%) as a yellow solid. 1H-NMR (400 MHz, Chloroform-d) delta 3.61 -3.72 (4H, m) , 3.75 -3.88 (4H , m) , 3.94 (3H, s) .

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.

Reference:
Patent; DIZAL (JIANGSU) PHARMACEUTICAL CO., LTD.; QI, Changhe; TSUI, Honchung; ZENG, Qingbei; YANG, Zhenfan; ZHANG, Xiaolin; (399 pag.)WO2020/35052; (2020); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

The chemical industry reduces the impact on the environment during synthesis 1458-18-0, name is Methyl 3-amino-5,6-dichloropyrazine-2-carboxylate, I believe this compound will play a more active role in future production and life. 1458-18-0

To a suspension of methyl 3-amino-5,6-dichloro-2-pyrazinecarboxylate (IVa) (5.55 g, 25.0 mmol) in 2-propanol (50 mL) was added hexamethyleneimine (2.73 g, 3.1 0 mL, 27.5 mmol) and the mixture was stirred at room temperature. Diisopropyethylamine (3.55 g, 4.79 mL, 27.5 mmol) was then added and the reaction mixture was heated at reflux. After 2 h the reaction was allowed to cool to room temperature, which caused the product to crystallize. The solid product was collected by vacuum filtration and washed with cold 2-propanol followed by diethyl ether. After drying, the desired product (Ilia) was obtained as pink crystals (5.91 g, 83%).

The chemical industry reduces the impact on the environment during synthesis 1458-18-0. I believe this compound will play a more active role in future production and life.

Reference:
Patent; UNIVERSITY OF WOLLONGONG; KELSO, Michael; RANSON, Marie; BUCKLEY, Benjamin; ABOELELA, Ashraf; (103 pag.)WO2018/81863; (2018); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

1458-18-0, 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. 1458-18-0 name is Methyl 3-amino-5,6-dichloropyrazine-2-carboxylate, This 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.

round bottomed flask was charged with methyl 6-amino 2,3-dichloro pyrazine 5-carboxylate (Aldrich, 25 g, 112.6 mmol), 2-S-ethyl piperazine (prepared as per Williams et al J. Med. Chem 1996, 39, 1345, 83% active, 15.7 g, 112.7 mmol), cesium carbonate (100 g, 300 mmol) and 1 ,4 dioxane (400 mL). The flask was equipped with a reflux condenser and heated to 8O0C. After 12hours the reaction was cooled, diluted with CH2CI2 (~ 200 mL), and filtered through celite. The filtrate was washed once with water and then concentrated to an oil. The crude product was purified by silica gel column chromatography (3% to 10% MeOH in CH2CI2) to afford compound A3 (30.8 g. 91 %). MS: M+H = 300

At the same time, in my other blogs, there are other synthetic methods of this type of compound, Methyl 3-amino-5,6-dichloropyrazine-2-carboxylate, and friends who are interested can also refer to it.

Reference:
Patent; SCHERING CORPORATION; PHARMACOPEIA DRUG DISCOVERY, INC.; WO2006/88836; (2006); A2;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – 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. 1458-18-0, name is Methyl 3-amino-5,6-dichloropyrazine-2-carboxylate, This compound has unique chemical properties. The synthetic route is as follows., 1458-18-0

The pyrazine (24.8 gm, 9.66 X 10″2 moles) was stirred in pyridine (200 mL) as benzoyl chloride (33.9 gm, 0.241 moles) was added in 3 portions. This solution was stirred at 65C overnight. After cooling, the pyridine was removed under reduced pressure and the remaining material was dissolved in methylene chloride (400 mL) and water (200 mL) was added. To this mixture was added potassium carbonate until the aqueous was basic to litmus. The methylene chloride solution was isolated and washed with 2% HCl (250 mL.). The solution was then dried over magnesium sulfate. After filtration, the solvents were removed under reduced pressure. The remaining material was stirred with diethyl ether (200 mL) causing the product to crystallize. The solid product was isolated by filtration. After washing with diethyl ether and drying the imide was obtained as a grey solid in a yield of 36.8 gm (82%).

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.

Reference:
Patent; JANUS BIOTHERAPEUTICS, INC.; LIPFORD, Grayson, B.; ZEPP, Charles, M.; WO2012/167046; (2012); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem