Process for the preparation of echinocandin derivatives

Abstract

A subject of the invention is a process for the preparation of the compounds of formula (I): R being as defined in the description as well as their salts, the intermediates, the use of the dihydrochloride as a medicament and the pharmaceutical compositions containing them. The process for preparing formula (I) leads to greater than 50% yield of isomer A, and its intended use, e.g. as an antifungal medicament.

1 . A compound of formula IIIa′:  
       
         
           
           
               
               
           
         
       
     
     
         2 . A compound of formula IV′:  
       
         
           
           
               
               
           
         
       
       where R represents a linear or branched or cyclic chain containing up to 30 carbon atoms, optionally containing one or more heteroatoms and one or more heterocycles.  
     
     
         3 . The compound of  claim 2 , having formulae IV′ containing an R radical selected from the following groups:  
       
         
           
           
               
               
           
         
       
     
     
         4 . A compound of formula IV′a  
       
         
           
           
               
               
           
         
       
       wherein R represents