PROCESS FOR PREPARING EPIRUBICIN AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF

摘要

PURPOSE: Provided is a process for preparing epirubicin and pharmaceutically acceptable salt thereof, thereby producing epirubicin in high yield and purity. CONSTITUTION: The preparing method of epirubicin represented by the formula(1) comprises the steps of: protecting 3'-amino group in saccharide region of doxorubicin to obtain a compound of the formula(2); ketalizing the compound of the formula(2) to obtain a compound of the formula(3); converting 4'- in saccharide region of the formula(3) to activated leaving group to obtain a compound of the formula(4); releasing the activated leaving group at 4'- to obtain a compound of the formula(5); hydrating 4'- in saccharide of the compound of the formula(5) to obtain a compound of the formula(6); and hydrating ketal derivative of aglycone to obtain a compound of the formula(1).