Patent ID: 6156911
Filing Date: 2000-12-05
Classification: C07D

Abstract:
A process for preparing a solution of purified lipstatin from a preparation containing lipstatin, one or more polar impurities and one or more non-polar impurities, comprising:a) mixing the preparation with a polar phase and a first non-polar phasewherein the first non-polar phase is a non-polar solvent selected from aliphatic hydrocarbons and aromatic hydrocarbons; and the polar phase is a polar solvent selected from carboxylic acids, alcohols, O-substituted monoethylene glycols, O-substituted oligoethylene glycols, O-substituted polyethylene glycols, diols, and dipolar aprotic solvents, wherein the polar solvent is undiluted or diluted with up to about twenty percent water;to form a first two phase system in which the ratio of the lipstatin to the non-polar impurities in the polar phase is greater than in the preparation,and separating the phases from the first two phase system and collecting the lipstatin-enriched polar phase, andb) diluting the lipstatin-enriched polar phase from step a) with water to form a diluted lipstatin-enriched polar phase containing the polar solvent in a percentage of at least seventy percent of the polar phase and lower than in the lipstatin-enriched polar phase from step a), and mixing the diluted lipstatin-enriched polar phase with a second non-polar phase, the second non-polar phase being the same non-polar solvent as the first non-polar phase in the same or greater relative amount to the polar phase as in the first two phase system;to form a second two phase system in which the ratio of the lipstatin to the polar impurities in the second non-polar phase is greater than in the lipid-enriched polar phase from step a),and separating the phases from the second two phase system and collecting the lipstatin-enriched second non-polar phase,thereby obtaining a lipstatin solution purified from the impurities present in the preparation.