Ethyl ({5-bromo-3-[(2-chloro-3,6-difluorobenzyl)amino]pyrazin-2-yl}amino)(oxo)acetate → 7-Bromo-1-(2-chloro-3,6-difluorobenzyl)-1,4-dihydropyrazino[2,3-b]pyrazine-2,3-dione

Participants

Reaction Steps

A solution of ethyl ({5-bromo-3-[(2-chloro-3,6-difluorobenzyl)amino]pyrazin-2-yl}amino)(oxo)acetate (1.20 g) in diglyme was heated at 165° C. for 16 hrs. The volatile components were removed on rotavap and then under vacuum. The residue was subjected to a silica gel column chromatography by using CH2Cl2/MeOH (9:1) as eluents, furnishing 7-bromo-1-(2-chloro-3,6-difluorobenzyl)-1,4-dihydropyrazino[2,3-b]pyrazine-2,3-dione in 43% yield (0.46 g).

Provenance & Evidence