6905-47-1

13484-56-5

General procedure for the synthesis of 2-amino-3-chloro-6-methoxypyrazine from 2-amino-6-methoxypyrazine: to a solution of 2-amino-6-methoxypyrazine (3 g, 24 mmol) in anhydrous N,N-dimethylformamide (DMF, 35 mL) was added N-chlorosuccinimide (NCS, 3.2 g, 24 mmol). The reaction mixture was stirred at room temperature for 16 h. After the reaction was completed, the mixture was poured into a mixture of ice and brine (130 mL). The aqueous phase was extracted with ethyl acetate (3 x 120 mL), the organic phases were combined, washed with 5% lithium chloride (LiCl) solution, dried over anhydrous sodium sulfate (Na2SO4) and concentrated under reduced pressure. The crude product was purified by SNAP-340-NH column chromatography (eluent: cyclohexane/ethyl acetate, gradient from 95:5 to 8:2) and SNAP1 00-Si-OH column chromatography (eluent: dichloromethane) to afford the target product, 2-amino-3-chloro-6-methoxypyrazine (1.98 g, 12.5 mmol, 52% yield). lc-MS (M-H) = 160.1.