Hydrochloric Acid → 3-Chloro-5,6,7,8-tetrahydroimidazo[1,2-a]pyrazine

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Reaction Steps

1,1-Dimethylethyl 3-chloro-5,6-dihydroimidazo[1,2-a]pyrazine-7(8H)-carboxylate (I19) (1.55 g, 6.01 mmol) and 4N HCl in 1,4-dioxane (6.01 mmol) was stirred at RT in 1,4-dioxane (5 mL) for 16 h. Solvents were removed in vacuo and the residue was loaded on to SCX (Varian 2×10 g) in methanol. The columns were washed with methanol and basic products eluted with 2M ammonia/methanol. The basic fractions were concentrated in vacuo to afford product in 913 mg that was used in subsequent steps without further purification.

Provenance & Evidence