Triethylamine → HCID 9953738, compound

Participants

Reaction Conditions

Reaction Steps

To the solution of 5,6-dimethyl-2-chloro4-(1-methyl- 1,2,3,4-tetrahydroisoquinolin-2-yl)pyrimidine (0.5 g, 1.74 mmol) prepared in accordance with WO 96/05177 in propylene glycol (2 ml), were added triethylamine (0.3 ml, 2.09 mmol) and 3,4-difluoroaniline (0.2 ml, 2.09 mmol). The reaction mixture was heated to 140° C., stirred for 18 hours, and cooled to room temperature. The resulting solution was diluted with dichloromethane, washed with water, and dried over anhydrous sodium sulfate. The organic layer was concentrated in vacuo. The resulting residue was subjected to silica gel column chromatography (eluent: ethyl acetate/hexane =⅓), and then treated with ethyl ether solution saturated with hydrochloric acid to afford 0.1 g (13.8%) of the titled compound.

Provenance & Evidence