Category: 1057216-55-3

1057216-55-3, name is 2-Chloro-5-iodopyrazine, belongs to pyrazines compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. SDS of cas: 1057216-55-3

Intermediate 31 (350 mg, 1.05 mmol), 2-chloro-5-iodopyrazine (252 mg, 1.05 mmol), 2M aqueous sodium carbonate solution (1.58 mL, 3.16 mmol) and anhydrous DMSO (5 mL) were charged to a sealed tube. The mixture was degassed by bubbling with nitrogen for 5 minutes before the addition of tetrakis(triphenylphosphine)20 palladium(0) (61 mg, 0.05 mmol). The reaction mixture was sealed under nitrogen andstirred at 110C for 1 h. The mixture was diluted with water (40 mL) and extracted with EtOAc (3 x 20 mL). The organic phase was washed with saturated aqueous sodium bicarbonate solution (2 x 10 mL) followed by brine (10 mL), then dried over sodium sulfate and concentrated under vacuum. The residue was purified by FCC, eluting with17-80% EtOAc in heptane, to afford the title compound (285 mg, 54% at 80% purity) as an off white solid. oH (500 MHz, CDC13) 8.73-8.64 (m, 2H), 8.63-8.59 (m, 1H), 7.92 (s, 2H), 7.33-7.27 (m, 1H), 7.17 (d, J8.2 Hz, 1H), 7.15-7.07 (m, 1H), 7.00 (d, J6.6 Hz, 1H),6.67 (t, J73.5 Hz, 1H), 4.36 (s, 2H), 2.60 (s, 3H). Method C HPLC-MS: MH+ m/z 401,

The synthetic route of 1057216-55-3 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; UCB PHARMA S.A.; BENTLEY, Jonathan Mark; BROOKINGS, Daniel Christopher; BROWN, Julien Alistair; CAIN, Thomas Paul; CHOVATIA, Praful Tulshi; FOLEY, Anne Marie; GALLIMORE, Ellen Olivia; GLEAVE, Laura Jane; HEIFETZ, Alexander; HORSLEY, Helen Tracey; HUTCHINGS, Martin Clive; JACKSON, Victoria Elizabeth; JOHNSON, James Andrew; JOHNSTONE, Craig; KROEPLIEN, Boris; LECOMTE, Fabien Claude; LEIGH, Deborah; LOWE, Martin Alexander; MADDEN, James; PORTER, John Robert; QUINCEY, Joanna Rachel; REED, Laura Claire; REUBERSON, James Thomas; RICHARDSON, Anthony John; RICHARDSON, Sarah Emily; SELBY, Matthew Duncan; SHAW, Michael Alan; ZHU, Zhaoning; WO2014/9295; (2014); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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. 1057216-55-3, name is 2-Chloro-5-iodopyrazine belongs to pyrazines compound, it is a common compound, a new synthetic route is introduced below. Product Details of 1057216-55-3

Step-a: Synthesis of 2-((5-iodopyrazin-2-yl)oxy)ethan-1-ol Into a 40-mL vial was placed 2-chloro-5-iodopyrazine (5.0 g, 20.80 mmol, 1.00 equiv), ethane-1,2-diol (3.36 g, 54.13 mmol, 2.60 equiv), sodium hydroxide (1.65 g, 41.25 mmol, 1.98 equiv), and NMP (5 mL). The resulting solution was stirred at 100 C. in an oil bath until completion. The reaction was then quenched by the addition of 200 mL water/ice. The solid was collected by filtration to deliver the title compound in 5.1 g (92%) as a light yellow solid. LCMS: 267 [M+H]+.

The synthetic route of 1057216-55-3 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; EISAI R & D MANAGEMENT CO., LTD.; BOCK, Mark; HAO, Ming-Hong; KORPAL, Manav; NYAVANANDI, Vijay Kumar; PUYANG, Xiaoling; SAMAJDAR, Susanta; SMITH, Peter Gerard; WANG, John; ZHENG, Guo Zhu; ZHU, Ping; MITCHELL, Lorna Helen; LARSEN, Nicholas; RIOUX, Nathalie; PRAJAPATI, Sudeep; REYNOLDS, Dominic; O’SHEA, Morgan; SAMARAKOON, Thiwanka; (134 pag.)US2018/141913; (2018); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Electric Literature of 1057216-55-3, The chemical industry reduces the impact on the environment during synthesis 1057216-55-3, name is 2-Chloro-5-iodopyrazine, I believe this compound will play a more active role in future production and life.

To a well stirred solution of 2-chloro-5-iodopyrazine (600 mg, 2.5 mmol), 3-fluorophenyl- acetylene (315 mg, 303 mu, 2.62 mmol, 1.05 equiv.) in 7 ml of THF were added under argon atmosphere bis(triphenylphosphine)-palladium(II)dichloride (175 mg, 0.250 mmol, 0.02 equiv.), copper(I) iodide (23.8 mg, 0.125 mmol, 0.01 equiv.) and triethylamine (556 mg, 761 ul, 5.49 mmol, 2.2 equiv.). The mixture was stirred for 2 hours at room temperature. The crude mixture was filtered, adsorbed on silicagel and purified by flash chromatography over a 50 g silicagel column using a heptane to 25% ethyl acetate in heptane gradient. The title compound (450 mg, 78% yield) was obtained as a crystalline light-yellow solid, MS: m/e = 233.1, 235.0 (M+H+).

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, 2-Chloro-5-iodopyrazine, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; F. HOFFMANN-LA ROCHE AG; GREEN, Luke; GUBA, Wolfgang; JAESCHKE, Georg; JOLIDON, Synese; LINDEMANN, Lothar; RICCI, Antonio; RUEHER, Daniel; STADLER, Heinz; VIEIRA, Eric; WO2011/128279; (2011); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

These common heterocyclic compound, 1057216-55-3, name is 2-Chloro-5-iodopyrazine, 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. Safety of 2-Chloro-5-iodopyrazine

Into a 250 ml round bottom flask, was placed isopropanol (150 ml). To the mixture was added XV-C-86 (5 g, 0.02 mol). To the mixture was added CuI (0.2 g, 1 mmol). To the mixture were added ethylene glycol (2.0 g, 0.03 mol), anhydrous potassium phosphate (6.5 g)and piperazine (1.3 g, 0.02 mol). The resulting solution was stirred, for 14 h while the temperature was maintained at 80-85 C. The resulting solution was concentrated in vacuo. To the residue was added 40 mL water and then extracted four times with 200 mL CH2Cl2. The organic layers were combined and dried with anhydrous sodium sulfate and concentrated in vacuo. The residue was purified by silica gel column chromatography. The collected fractions were combined and concentrated in vacuo to afford XV-D-86.

The synthetic route of 2-Chloro-5-iodopyrazine has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Kalypsys, Inc.; US2005/234046; (2005); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

1057216-55-3, name is 2-Chloro-5-iodopyrazine, belongs to pyrazines compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. Recommanded Product: 2-Chloro-5-iodopyrazine

Intermediate 31 (350 mg, 1.05 mmol), 2-chloro-5-iodopyrazine (252 mg, 1.05 mmol), 2M aqueous sodium carbonate solution (1.58 mL, 3.16 mmol) and anhydrous DMSO (5 mL) were charged to a sealed tube. The mixture was degassed by bubbling with nitrogen for 5 minutes before the addition of tetrakis(triphenylphosphine)20 palladium(0) (61 mg, 0.05 mmol). The reaction mixture was sealed under nitrogen andstirred at 110C for 1 h. The mixture was diluted with water (40 mL) and extracted with EtOAc (3 x 20 mL). The organic phase was washed with saturated aqueous sodium bicarbonate solution (2 x 10 mL) followed by brine (10 mL), then dried over sodium sulfate and concentrated under vacuum. The residue was purified by FCC, eluting with17-80% EtOAc in heptane, to afford the title compound (285 mg, 54% at 80% purity) as an off white solid. oH (500 MHz, CDC13) 8.73-8.64 (m, 2H), 8.63-8.59 (m, 1H), 7.92 (s, 2H), 7.33-7.27 (m, 1H), 7.17 (d, J8.2 Hz, 1H), 7.15-7.07 (m, 1H), 7.00 (d, J6.6 Hz, 1H),6.67 (t, J73.5 Hz, 1H), 4.36 (s, 2H), 2.60 (s, 3H). Method C HPLC-MS: MH+ m/z 401,

The synthetic route of 1057216-55-3 has been constantly updated, and we look forward to future research findings.