Several efficient new methods for synthesizing rhenium compounds conta
ining a multiply bonded imido linkage (Re=N-R) between the metal and o
rganic compounds for radiopharmaceutical applications are reported. Th
e imido linkage is stable and compatible with typical organic function
al groups, and offers distinct structural and synthetic advantages ove
r other types of linkages commonly used in radiopharmaceutical design.
Syntheses of representative peptide and steroid compounds from hydraz
ine and phosphinimine imido precursors are described, and the preparat
ion of a Re-188-imido complex is discussed. A promising new Re-188-rad
iolabeling strategy for directly synthesizing rhenium imido radiopharm
aceuticals, targeted for low-capacity receptor sites relevant for canc
er therapy and based on solid supported imido precursors, is presented
.