PROCESS FOR THE PRODUCTION OF BENDAMUSTINE ALKYL ESTER, BENDAMUSTINE, AND DERIVATIVES THEREOF

摘要

The invention relates to a method for the production of bendamustine alkyl ester, bendamustine, as well as derivatives thereof. With the method according to the invention, the production of these compounds is possible in reproducibly high yields. To this end, hydroxyl-group- containing esters are used as the starting material whose hydroxyl groups are substituted in a simple way by halogen groups. This substitution is possible in the presence of (i) oxalyl chloride and (ii) dialkylformamide, dialkyl acetamide or dimethyl sulfoxide. In a subsequent reaction, the resulting esters can be hydrolyzed to form acid.