Piperazine → 1-(3-Methoxypyridin-2-yl)piperazine

Participants

Reaction Steps

Anhydrous piperazine (45.6 g) and 2-bromo-3-methoxypyridine (10.0 g) were heated neat in an autoclave at 100° C. for 20 h. Upon cooling, the mixture was treated with 5% NaCO3 (20 mL) and extracted with CH2Cl2 (3×50 mL). The extracts were dried using anhydrous K2CO3, filtered, and concentrated under reduced pressure to yield 1-(3-methoxy-2pyridinyl)piperazine (III; 8.43 g; 82%) after silica gel chromatography (CH2Cl2/MeOH/NH4OH; 93:7:0.7).

Provenance & Evidence