Patent ID: 6153756
Filing Date: 2000-11-28
Classification: C07D

Abstract:
A method of producing a 2'-onium salt of paclitaxel having the following formula: ##STR4## wherein X.sup.- is CH.sub.3 SO.sub.3.sup.-, H.sub.2 PO.sub.4.sup.- or HCO.sub.3.sup.-, said method comprising:a) forming a mixture by dissolving paclitaxel and a 2-halo-1-onium tosylate salt in a substantially dry organic solvent;b) adding a quaternary compound forming agent to the mixture;c) stirring or agitating the mixture and evaporating it to leave a dry residue;d) dissolving the dry residue in a second organic solvent to produce a solution suitable for high performance liquid chromatography (HPLC);e) chomatographing the solution by reverse phase HPLC in an HPLC column using a mixture of said second solvent and water as a first mobile phase for an initial period during which all fractions other than those containing the desired onium salt end product are eluted from the column; andf) causing the fractions containing the desired onium salt product to elute from the column by using as a second mobile phase a solution of NaX in a mixture of said second solvent and water, wherein X is defined as above.