Hydrogen Bromide → 8-Chloroimidazo[1,2-a]pyrazine

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Reaction Steps

HBr (48% in H2O) is added to a solution of 2-amino-3-chloropyrazine (1.2 g, 9.26 mmol) and BrCH2CH(OEt)2 (1.6 mL, 10 mmol) in MeOH and H2O (5 mL and 10 mL) at RT. The mixture is stirred for 24 h at RT and then heated to 40° C. for 48 h. The pH is adjusted to 7 with sat. Na2CO3. The mixture is extracted with CH2Cl2. The organic phase is dried over anhydrous Na2SO4. The product is purified by silica gel column chromatography (4% MeOH in CH2Cl2) to give the title compound as an off white solid.

Provenance & Evidence