A novel process for the preparation of ibodutant (MEN15596).

Abstract

This invention relates to a novel process for synthesising the product ibodutant shown in the figure below, consisting of a small number of highyield steps involving reagents and solvents with low environmental impact, characterised by the coupling of two portions, compounds (3) and (4), one of which (3) is synthesised by coupling of 6methy1-2- benzo[b]thiophenecarboxylic acid (1) with 1-amino-alpha-alpha-cyclopentan carboxylic acid and subsequent cyclization with oxazolone, while the other, compound (4), is obtained from suitable highly selective functionalisations of 4aminomethy lpiperidine (2)