反应详情

To a solution cooled to about 0° C. of 5.99 g (15.9 mmol) of tert-butyl 8-carbamoyl-6-chloro-7-phenyl-3,4-dihydropyrrolo[1,2-a]pyrazine-2(1H)-carboxylate in 50 ml of dichloromethane and 200 ml of methanol are added portionwise 12.6 g (116 mmol) of chlorotrimethylsilane. The mixture is stirred for 16 hours at room temperature and the reaction medium is then concentrated under reduced pressure and co-evaporated twice with ethyl acetate. The residue is crystallized from ethyl acetate to give 4.88 g of 6-chloro-7-phenyl-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine-8-carboxamide hydrochloride in the form of a white solid after drying at 60° C. under reduced pressure.

1. concentrationthe reaction medium is then concentrated under reduced pressure
2. customThe residue is crystallized from ethyl acetate