Synthesis of 4'-epi-iodo-4'-deoxy-daunorubicin, a potential cancer radiotherapeutic agent

Article abstract of DOI:10.1016/S0960-894X(98)00616-7

We have prepared 4'-epi-iodo-4'-deoxy-daunorubicin (IDDNR)(1), a doxorubicin analog, via a 5-step synthesis involving a protected daunorubicin triflate derivative (4). This triflate derivative will allow the facile and regiospecific nucleophilic preparation of I-125 or Br-80m labelled analogs of IDDNR. Auger electronemitting I-125- or Br-80m-labelled analogs of IDDNR may have potential as cancer radiotherapeutic agents.