Sodium Carbonate → Tert-butyl 4-(6-chloropyrazin-2-YL)piperazine-1-carboxylate

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Reaction Steps

A mixture of 2,6-dichloropyrazine (2.98 g, 20 mmol), piperazine-1-carboxylic acid tert-butyl ester (3.72 g, 20 mmol) and sodium carbonate (2.12 g, 20 mmol) in t-butanol (50 mL) was heated at reflux under nitrogen for 65 h. The solution was concentrated in vacuo. The residue was partitioned between ethyl acetate (50 mL) and water (50 mL). The aqueous phase was extracted with ethyl acetate (3×30 mL). The combined organic extracts were washed with brine (50 mL), dried over magnesium sulfate, filtered, and concentrated in vacuo to give the title compound (I-1a) as a white solid.

Provenance & Evidence