2-Chloropyridine → (3R)-3-methyl-1-pyridin-2-ylpiperazine

Participants

Reaction Steps

To a solution of (R)-2-methyl piperazine (6.6 g, 0.066 mol) in xylene (100 mL) at 140° C. under nitrogen was added 2-chloro pyridine (4 g, 0.035 mol) slowly over a period of 1 h. The heating was continued for additional 12 h and cooled to RT. The solvent was removed under reduced pressure and the resulting residue was purified by chromatography using chloroform methanol (8/2) as eluent to afford the title product as a liquid (2.5 g, 40%). TLC-Chloroform/MeOH (8/2); Rf=0.2. HPLC purity: 97%.

Provenance & Evidence