Patent ID: 8664409

Claim:
A process for the preparation of a (poly)aminoalkylaminoacetamide derivative of epipodophyllotoxin, of formula 1 or a pharmaceutically acceptable salt thereof, wherein R represents a hydrogen atom or a group —(CH 2 ) c —NH 2 , wherein a, b and c each independently represent 2, 3, 4 or 5, comprising peptide coupling of 4-amino-4′-demethylepipodophyllotoxin of formula 4bis with a compound of formula 6 wherein P represents a protecting group for the amine function selected from benzyloxycarbonyl and t-butyloxycarbonyl, and R′ represents H or a chain —(CH 2 ) c —NHP, wherein c represents 2, 3, 4 or 5, wherein O-benzotriazol-1-yl-N,N,N′,N′-tetramethyluronium tetrafluoroborate (TBTU) is employed as a coupling agent, and wherein the coupling reaction is performed without using an excess of reactant.