13-DEOXYANTHRACYCLINE DERIVATIVES AND PROCESSES FOR PREPARING THEM

摘要

A high yeld process for preparing 13-deoxyanthracycline derivatives as anticancer of low cardio toxicities, includes the steps of: forming a solution of anthracycline 13-tosylhydrazone; adding a reducing agent to reduce the 13-keto moiety to a methylene moiety; refluxing the solution; cooling the reaction mixture; adding saturated aqueous NaHCO 3 ; adding a halocarbon solvent to the reaction mixture; filtering the reaction mixture; acidifying the filtrate; and subjecting the filtrate to chromatography to isolate the 13-deoxyanthracycline derivatives.