Process for the preparation of ibodutant (MEN15596) and related intermediates

摘要

This invention relates to a novel process for synthesising the product ibodutant shown in the figure below, consisting of a small number of high- yield 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 6-methyl-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 4-aminomethylpiperidine (2).