| abstract |
Disclosed is a process for the preparation of (poly)aminoalkylaminoacetamide derivatives of epipodophyllotoxin, of formula 1, or a pharmaceutically acceptable salt thereof, and products produced by the process. R represents a hydrogen atom or a group -(CH2)c-NH2, and 2 ? a,b,c ? 5, comprising a step of condensation of 4beta-chloroacetamido-4'-demethylepipodophyllotoxin of formula 4 with a primary-amine-containing reactant of formula 6, where the amine functional groups of formula 6 are not protected. An example of the compounds produced by this method include 2-{ 3-[4-(3-aminopropylamino)-butylamino]-propylamino} -N-[9-(4-hydroxy-3,5-dimethoxyphenyl)-S-oxo-5,5a,6,S,Sa,9-hexahydrofuro[3',4':6,7]naphtho[2,3-d][1 ,3]dioxol-5-yl]-acetamide. |