Some common heterocyclic compound, 1062608-42-7, name is 5-Bromo-3-iodopyrazin-2-amine, molecular formula is C4H3BrIN3, 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 5-Bromo-3-iodopyrazin-2-amine
To the solution of compound (iii) (355 mg, 1.18 mmol) in 1,4-dioxane (5 ml) was added a boronic acid of formula (iv) such as 6-methoxypyridin-3-yl boronic acid (CombiB locks 190 mg, 1.24 mmol) at RT and the reaction mixture was purged with N2 gas for 30 minutes. Bis(triphenylphosphine)palladium(II)chloride (58 mg, 0.08 mmol) and 1 M aqueous solution of potassium carbonate (1.42 ml, pre-purged with N2 gas) were added to the reaction mixture. The solution was heated to reflux for 16 h and then cooled to RT, added Brine solution (5 ml) and extracted with ethyl acetate (10 ml X 4). Combined organic layers were dried over anhydrous Na2S04 and concentrated. Crude material was purified by column chromatography over silica gel 230-400 mesh by using 1-2% MeOH in DCM as an eluent to yield compound (v) (150 mg, 45.18%) as solid.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 1062608-42-7, its application will become more common.
Reference:
Patent; UNIVERSITY OF CAPE TOWN; MMV MEDICINES FOR MALARIA VENTURE; YOUNIS, Yassir; CHIBALE, Kelly; WITTY, Michael, John; WATERSON, David; WO2013/121387; (2013); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem