Process for the preparation of 10-deacetylbaccatin III

摘要

The present invention discloses a process for the conversion of a mixture of taxol analogues 7-xylosyl-10-deacetylbaccatin taxols of the formula 2 <CHEM> where R is C6H5, CH3C=CHCH3 or C5H11 into 10-deacetylbaccatin III of the formula 1 <CHEM> by dissolving the taxol analogue of formula 2 in a polar solvent, reacting the resultant solution with a base, and isolating 7-xylosyl-10-deacetylbaccatin III, dissolving the 7-xylosyl-10-deacetylbaccatin III in a polar solvent, reacting the resultant solution with a periodate to cleave the diol system of the xyloside into dialdehyde, treating the generated dialdehyde in an organic acid medium with an amine salt and isolating 10-deacetylbaccatin III of formula 1.