Benzylamine → N-benzyl-6-(4-methylpiperazin-1-yl)-3-nitropyridin-2-amine

Participants

Reaction Conditions

Reaction Steps

2,6-Dichloro-3-nitropyridine E-3.1″(1.5 g; 7.151 mmol) is suspended in NMP and cooled to 0° C. DIPEA (2.31 ml, 14.3 mmol) and benzylamine (800 μl; 7.47 mmol) are added, the reaction mixture is stirred at RT. To this suspension 1-methylpiperazine (875 μl; 7.87 mmol) is added and the resulting mixture is stirred for 16 h at 50° C. The crude intermediate is purified using reversed phase chromatography (prep. HPLC1). The product containing fractions are combined and freeze-dried (Yield: 49%; 1.144 g; 3.494 mmol)

Provenance & Evidence