Alkylation of 7-ethyl-10-hydroxycamptothecin (I) with 1,2-dibromoethane (II) under Williamson's ether synthesis conditions furnished the bromoethyl ether (III). Subsequent regioselective nitration of (III) provided the desired 9-nitro compound (IV), which was further reduced to the corresponding amine (V) by using SnCl2 in concentrated HCl. Finally, cyclization of the bromo amine (V) to give the title hexacyclic compound was carried out either in the presence of KI and K2CO3 in refluxing acetone or on standing in a DMSO solution at room temperature.