3,4-Dichloro-2-(hydroxymethyl)pyridine → 2-[(3-Chloro-2-hydroxymethyl-pyridin-4-yl)-methylamino]-ethanol

Participants

Reaction Steps

A mixture of 3,4-dichloro-2-hydroxymethylpyridine (J. Med. Chem. 1989, 32, 1970) (2.5 g) in 2-methylaminoethanol (30 ml) is heated at 160° C. in a steel autoclave for 2.5 h, the excess amine is stripped off under high vacuum, and the remaining residue is chromatographed on silica gel (dichloromethane/methanol 95/5). Yield: 2.3 g as yellowish oil.

Provenance & Evidence