(3R)-1-methylpiperidin-3-ol → (1R/S,3R)-3-Hydroxy-1-(isoxazol-3-ylcarbamoylmethyl)-1-methyl-piperidinium bromide

Participants

Reaction Steps

(R)-1-Methyl-piperidin-3-ol (1.15 g, 10 mmol) and 2-bromo-N-isoxazol-3-yl-acetamide (Intermediate A) (2.25 g, 11 mmol) are stirred together in chloroform/acetonitrile (20 ml of a 1:1 mixture) at room temperature for 1 hour. The solvent is removed in vacuo and the resulting oil is purified using C-18 reverse phase column chromatography (eluent-water:acetonitrile from 0% to 30% acetonitrile) to yield the titled compound.

Provenance & Evidence