The present invention concerns a process for the preparation of naldemedine or a salt thereof, comprising the steps of: a) reacting naltrexone (II) and diethyl pyrocarbonate (DEPC) and treating with a base to give compound (III); b) condensing compound (III) with compound (IV) with formation of the amide bond to obtain naldemedine (I). The process according to the present invention is therefore very simple, effective, and industrially applicable, and above all cost-effective, since it avoids the steps of protection and deprotection of the phenolic group of the structures involved.
PROCESS FOR THE PREPARATION OF NALDEMEDINE
BAUDINO MATTEOFirst
;
2023-01-01
Abstract
The present invention concerns a process for the preparation of naldemedine or a salt thereof, comprising the steps of: a) reacting naltrexone (II) and diethyl pyrocarbonate (DEPC) and treating with a base to give compound (III); b) condensing compound (III) with compound (IV) with formation of the amide bond to obtain naldemedine (I). The process according to the present invention is therefore very simple, effective, and industrially applicable, and above all cost-effective, since it avoids the steps of protection and deprotection of the phenolic group of the structures involved.
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