Diisopropylethylamine → (R)-(1-(6-amino-5-nitropyridin-2-yl)piperidin-3-yl)(pyrrolidin-1-yl)methanone

Participants

Reaction Conditions

Reaction Steps

A solution of 6-chloro-3-nitropyridin-2-amine (0.175M, 20 mL, 3.5 mmol) in anhydrous N,N-dimethylformamide was added to (R)-piperidin-3-yl(pyrrolidin-1-yl)methanone, followed by diisopropylethylamine (1.3 mL, 7.0 mmol). The reaction mixture was stirred at 80° C. for 16 h. The solvent was removed under reduced pressure and the residue was purified via preparative HPLC to afford (R)-(1-(6-amino-5-nitropyridin-2-yl)piperidine-3-yl)(pyrrolidin-1-yl)methanone (1.0 g, 89.6%).

Provenance & Evidence