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

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...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1998-12, Vol.8 (23), p.3419-3422
Hauptverfasser:	Murali, Dhanabalan, DeJesus, Onofre T.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antibiotics, Antineoplastic - chemical synthesis Biological and medical sciences Contrast media. Radiopharmaceuticals Daunorubicin - analogs & derivatives Daunorubicin - chemical synthesis Intercalating Agents - chemical synthesis Iodine Radioisotopes - therapeutic use Medical sciences Neoplasms - radiotherapy Pharmacology. Drug treatments
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Zusammenfassung:	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 electron-emitting I-125- or Br-80m-labelled analogs of IDDNR may have potential as cancer radiotherapeutic agents. Synthesis of 4′- epi-iodo-4′-deoxy-daunorubicin ( 1) via a 5-step synthesis involving 4 is described.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(98)00616-7