Hydrazine hydrate (1:1) → (r)-{1-[(1-{2-[4-(2-Aminoethyl)phenyl]ethyl}piperidin-4-yl)methyl]-1h-1,2,4-triazol-3-yl}(cyclohexyl)phenylmethanol

Participants

Reaction Steps

2-[2-(4-{2-[4-({3-[(R)-cyclohexyl(hydroxy)phenylmethyl]-1H-1,2,4-triazol-1-yl}methyl)piperdin-1-yl]ethyl}phenyl)ethyl]-1H-isoindole-1,3(2H)-dione (Preparation 12, 3.4 g, 5.38 mmol) was suspended in ethanol (20 ml) and hydrazine monohydrate (2.61 ml, 53.8 ml) added. After stirring at reflux for 2 hours, the reaction was cooled to room temperature and the precipitate collected by filtration and washed with ethanol (200 ml). The filtrate was concentrated in vacuo to furnish the title compound as a white solid, in 81% yield, 2.57 g.

Provenance & Evidence