Acetonitrile → 2-[(3S)-3-Aminopyrrolidin-1-yl]-6-chloro-N-[(1-hydroxycycloheptyl)methyl]-quinoline-5-carboxamide

Participants

Reaction Steps

(S)-3 aminopyrrolidine (96 ml) and acetonitrile (300 ml) were charged to a vessel containing 2,6-Dichloro-N-((1-hydroxycycloheptyl)methyl)quinoline-5-carboxamide (300.0 g), potassium carbonate (249.0 g) and acetonitrile (2400 ml). The reaction mixture was heated under refux for 20 hours. Water (6900 ml) was charged at 20° C. to 25° C. The mixture was stirred for 95 minutes and filtered. The filter cake was washed with water (1200 ml) and acetonitrile (1200 ml). The filter cake was dried at 40° C. for 48 hours to provide the title compound as a yellow solid (283 g).

Provenance & Evidence