Hydrazine hydrate (1:1) → HCID 68495857, compound

Participants

Reaction Steps

In analogy to Wermuth et al. in J. Med. Chem. 1987, 30 (2), 246, hydrazine hydrate (10 mL) was added to a solution of 4-(1-isopropylpiperidin-4-yl)-2-morpholin-4-yl-4-oxo-butyric acid (99.9 g, 0.25 mol) in 2-butanol (500 mL). The reaction mixture was stirred at room temperature for 1 h followed by reflux overnight. After cooling to room temperature the solvent was evaporated under reduced pressure. The residue was purified by flash column chromatography (SiO2, dichloromethane with 3% methanol followed by 5% and 7%.). Evaporation of the fractions containing the desired product yielded a yellow solid, which was used as such.

Provenance & Evidence