M. Scobie et Md. Threadgill, TUMOR-TARGETED BORANES .3. SYNTHESIS OF CARBAMATE-LINKED NITROIMIDAZOLYL CARBORANES DESIGNED FOR BORON NEUTRON-CAPTURE THERAPY OF CANCER, Journal of the Chemical Society. Perkin transactions. I, (15), 1994, pp. 2059-2063
Carboranes targetted to specific tumour tissues are important for boro
n neutron capture therapy of cancer (BNCT), Carbamoylation of -[2-[2-(
2-nitroimidazol-1-yl)ethoxy]ethoxy]ethanol 5 and 1-(chloromethyl)-2-(2
-nitroimidazol-1-yl)ethanol 6 with carboran-1-yl isocyanate (generated
in situ by a Curtius rearrangement of carborane-1-carbonyl azide) gav
e the corresponding carbamate-linked nitroimidazolylcarboranes 16 and
17. A similar reaction of 4-carboranylphenyl isocyanate with 6 afforde
d the corresponding carbamate 24.