发明申请
US20160137683A1 Method for Preparing Epirubicin and Intermediate Thereof 有权
制备表柔比星及其中间体的方法

Method for Preparing Epirubicin and Intermediate Thereof
摘要:
The present invention provides a method for preparing epirubicin and an intermediate adaptive to the method. The preparation method may include: reacting tert-Butyldimethylsilyl chloride with N-trifluoroacetyl adriamycin to obtain a first compound N-trifluoroacetyl-14-O-tert-Butyldimethylsilyl adriamycin; oxidizing the first compound to obtain a second compound 4′-ketone-N-trifluoroacetyl-14-O-tert-Butyldimethylsilyladriamycin; reducing the second compound to obtain a third compound N-trifluoroacetyl-14-O-tert-Butyldimethylsilyl epirubicin; and performing deprotection and hydrolysis reactions on the third compound to obtain epirubicin. The method of the present invention needs low cost, fewer reaction steps, provides high yield and high product purity, and avoids serious pollution caused by a bromination reaction in a conventional method.
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