The reaction of 2'-O-(triethylsilyl)paclitaxel (I) with dimethyl sulfide (DMS) and Bz2O2 in acetonitrile gives the 7-O-(methylsulfanylmethyl) derivative (II), which is condensed with chloroacetic acid (III) by means of N-iodosuccinimide (NIS) and Ag-OTf in THF to yield the 7-O-(chloroacetoxymethyl) derivative (IV). The desilylation of (IV) by means of HCl in acetonitrile affords the intermediate (V), which is finally condensed with the secondary amine (VI) by means of NaI in acetone to provide the target hybrid molecule.