Hydrochloric Acid → 2-(Azetidin-3-YL)-3-chloropyrazine hydrochloride

Participants

Reaction Steps

To a solution of tert-butyl 3-(3-chloropyrazin-2-yl)azetidine-1-carboxylate (7) (300 g, 1.112 mol, 1 eq.) in methanol (6 L) was added concentrated HCl (400 mL, 4.8 mol, 4.3 eq.) and the resulting mixture was stirred at RT for 112 h. The mixture was concentrated and dried on rotavapor to obtain 230 g of 2-(azetidin-3-yl)-3-chloropyrazine hydrochloride (8).

Provenance & Evidence