Research on new synthetic routes about 5,8-Dibromoimidazo[1,2-a]pyrazine

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.

Application of 957344-74-0, A common heterocyclic compound, 957344-74-0, name is 5,8-Dibromoimidazo[1,2-a]pyrazine, molecular formula is C6H3Br2N3, 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.

Step 1 4-(5-Bromoiotamiotadazo[l,2-a]pyraziotan-8-ylamiotano) benzoic acid methyl ester[00266] A mixture of 5,8-dibromoimidazo[l,2-a]pyrazme (2g, 7 3mmol), 4-amino benzoic acid methyl ester (0 93g, 6 2mmol), NaO’Bu (0 98g, 10 2mmol), Pd2(dba)3 (133mg, 0 14mmol), Xantphos (168mg, 0 29mmol) and toluene is degassed with nitrogen, then heated at 850C for 18 hours The toluene is removed in vacuo, then MeOH is added to the crude residue The solid is collected by filtration and dried in the vacuum oven The solid is identified as the desired title ester The filtrate is chromatographed with petrol EtOAc (70 30 followed by 50 50) and the fractions containing the desired product, combined, evaporated and triturated with MeOH The resultant solid is collected by filtration and is also identified as the desired ester

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.

Reference:
Patent; GALAPAGOS N.V.; WO2007/131991; (2007); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem