Water → 1-(6-Methoxypyridin-3-YL)piperazine

Participants

Reaction Steps

A mixture of 6-methoxy-3-pyridinamine (0.2 mol) and 2-chloro-N-(2-chloroethyl)-ethanamine hydrochloride (0.3 mol) in 2-butanol (500 ml) was stirred and refluxed. Potassium carbonate (0.7 mol) was added portionwise (20 g/h), the mixture was refluxed for 48 hours, an additional amount of potassium carbonate (30 g) was added and the mixture was stirred for 48 hours. The mixture was poured into water, extracted with CH2Cl2 and separated. The organic layer was dried, filtered and evaporated, yielding 38 g (98%) of 1-(6-methoxy-3-pyridinyl)piperazine (interm. 29).

Provenance & Evidence