Patent ID: 8431684

Claim:
Process for the preparation of the compound ibodutant which comprises: a) preparing the intermediate (12) through the following steps: a′) protection of the primary amine of 4-aminomethyl-piperidine (2) with ethyl-trifluoroacetate, followed by reductive amination of protected 4-aminomethyl-piperidine with 4-formyl-tetrahydropyran and a borane and by deprotection in basic medium to yield the intermediate diamine (11) b′) reaction of the diamine (11) with Boc-D-Phe to give the intermediate (12) or alternatively through the following steps: a″) reaction between 4-aminomethyl-piperidine (2) and Boc-D-Phe(OSu) to yield the intermediate (17) b″) reductive amination of (17) with 4-formyl-tetrahydropyran and a borane to give the intermediate (12), b) deprotection of the intermediate (12) to yield (4) c) reaction between (4) and the compound (3) thereby obtaining the final product.